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Metabolism PDE

PDE

A phosphodiesterase (PDE) is an enzyme that breaks a phosphodiester bond. Usually, phosphodiesterase refers to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases (which all break the phosphodiester backbone of DNA or RNA), as well as numerous less-well-characterized small-molecule phosphodiesterases.The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators of signal transduction mediated by these second messenger molecules.
Cat No. product name
T0045 Heptaminol hydrochloride Heptaminol hydrochloride, a vasoconstrictor, is used in the therapy of hypotension, especially orthostatic hypotension.
T0070 Pentoxifylline Pentoxifylline modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase ...
T0080 Trapidil Trapidil is a coronary vasodilator agent. It was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic...
T0096 Vardenafil Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific...
T0160 Anagrelide Anagrelide is a Platelet-reducing Agent. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by...
T0167 Vinpocetine Vinpocetine is a selective inhibitor of cyclic GMP phosphodiesterase (PDE).
T0264 Zomepirac Sodium Zomepirac sodium salt is a prostaglandin synthetase inhibitor.
T0383 Fenspiride hydrochloride Fenspiride, an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of ...
T0458 Indometacin Indomethacin is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of indomethacin is as a Cyclooxygenase Inhibitor.
T0462 Cilostazol Cilostazol is a Phosphodiesterase 3 Inhibitor. The mechanism of action of cilostazol is as a Phosphodiesterase 3 Inhibitor.
T0467 Sildenafil citrate Sildenafil, a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less co...
T0480 Doxofylline Doxofylline is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has show...
T0625 Theobromine 3, 7-Dimethylxanthine, a xanthine alkaloid, is used as a bronchodilator and as a vasodilator.
T0705 Triflusal Triflusal is a 2-acetoxy-4-trifluoromethylbenzoic acid and it is an aspirin chemically-related molecule but not a derivative.
T0892 Diprophylline Dyphylline is a xanthine derivative. Dyphilline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Dyphilline prob...
T0994 Ketotifen fumarate Ketotifen is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.
T1024 Roflumilast Roflumilast is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activiti...
T1027 Luteolin Luteolin is a naturally occurring flavonoid. The flavonoids are polyphenolic compounds found as integral components of the human diet. In vitro work has concent...
T1056 Isoprenaline hydrochlorideHOT Isoproterenol is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
T1083 Theophylline Theophylline is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant ac...
T1083L Theophylline monohydrate Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize ade...
T1096 Milrinone Milrinone is a Phosphodiesterase 3 Inhibitor. The mechanism of action of milrinone is as a Phosphodiesterase 3 Inhibitor.
T1112 2-(Hydroxymethyl)pyridine 2-Pyridinylmethanol is an organic compound.
T1164 Sildenafil Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor, used to treat erectile dysfunction and reduce symptoms of pulmonary arterial hypertension (PAH).
T1265 Amrinone Amrinone is a positive inotropic cardiotonic (cardiotonic agent) with vasodilator properties, phosphodiesterase 3 inhibitory activity.
T1398 Tadalafil Tadalafil is a carboline-based compound with vasodilatory activity. Tadalafil selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 pho...
T1618 Dypyridamole Dipyridamole is a Platelet Aggregation Inhibitor. The physiologic effect of dipyridamole is by means of Decreased Platelet Aggregation.
T1681 Aminophylline Aminophylline is a competitive nonselective phosphodiesterase inhibitor giving a bronchodilatory effect.
T1708 Pimobendan Pimobendan is a selective inhibitor of PDE3 (IC50: 0.32 μM).
T1713 IBMXHOT IBMX is a pan-phosphodiesterase (PDE) inhibitor (IC50s: 6.5/26.3/31.7 μM for PDE3/PDE4/PDE5).
T1745 TAK063 TAK-063 is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs.
T2129 Zaprinast Zaprinast was an unsuccessful Clinicalal drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which succe...
T2137 Ibudilast Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor. It is approved for use as an anti-inflammatory in Japan.
T2205 Theophylline-7-acetic acid Theophylline-7-acetic acid, a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in th...
T2334 Avanafil Avanafil is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction.
T2855 Icariin Icariin is a flavonol glycoside, inhibiting PDE5 and PDE4 activities. Icariin also is a PPARα activator.
T2923 Apremilast Apremilast (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.
T3631 PF8380 PF-8380 is an effective and orally available autotaxin inhibitor (IC50: 2.8 nM, in isolated enzyme assay; 101 nM, in the human whole blood). It modulates lysoph...
T3987 Lotamilast E6005 is a phosphodiesterase 4 (PDE-4) inhibitor (IC50: 2.8 nM) potentially for the treatment of atopic dermatitis.
T4041 GLPG1690 GLPG-1690, an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.
T4097 Vardenafil hydrochloride trihydrate Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
T6042 PF-2545920 PF-2545920, a specific and effective PDE10A inhibitor (IC50=0.37 nM), is with more than1000-fold specificity activity over the PDE.
T6054 GSK256066 GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380, 000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold sele...
T6390 Anagrelide HCl Anagrelide Hydrochloride(BL4162A) is a drug used for the treatment of essential thrombocytosis.
T6445 Cilomilast Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.
T6462 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
T6548 Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
T6644 Rolipram Rolipram is a phosphodiesterase 4 inhibitor with antidepressant properties.
T6649 S- (+)-Rolipram S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous...
T6983 Sildenafil Mesylate Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
T4285 Crisaborole AN-2728 is a Phosphodiesterase 4 Inhibitor.
T4S0792 (+)-pinoresinol-β-D-glucoside; (+)-pinor
T4695 CP671305 CP671305 is an orally active, potent and selective inhibitor of phosphodiesterase-4-D.
T5106 BRL 50481 BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.
T5033 Olprinone Olprinone(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor.Olprinone has been reported to improve microcirculation and attenuate inflammation. Olp...
T5101 BW-A78U BW-A 78U is a PDE4 inhibitor (IC50: 3 μM). It is not inhibition on the lipopolysaccharide (LPS)-induced TNF-α release.
T6S2115 Ginkgolide J Ginkgolide J has neuroprotective activity, it can prevent A beta(1-42) induced inhibition of long-term potentiation in the CA1 region of mouse hippocampal slice...
T5411 SEP-0372814 PDE10-IN-1 is PDE10-IN-1 inhibitor extracted from Patent WO 2013192273 A1, for treating CNS and metabolic disorders.
T5474 D 159687 D159687 is a selective PDE4D inhibitor,had a procognitive profile as it improved memory in the novel object recognition test but had no antidepressant or anxi...
T5956 VP3.15 dihydrobromide VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE7- glycogen synthase kinase (GSK)3 inhibitor(with IC50s of 1...
T6147 Nortadalafil Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, treating erectile dysfunction (ED) ; and under the name Adcirca for the treatment of pulmonary ar...
T5940 Proxyphylline Proxyphylline is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and...
T7346 Lodenafil Lodenafil is a potent PDE5 inhibitor, with treatment of erectile dysfunction (ED)
T7542 Amino Tadalafil Amino tadalafil is a potent phosphodiesterase 5 (PDE5) inhibitor.
T7642 Cilostamide Cilostamide is a selective phosphodiesterase (PDE)3A and PDE3B inhibitor(IC50 values of 27 and 50 nM, respectively)
TQ0126 Mirodenafil dihydrochloride Mirodenafil (SK3530) dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.
T3224 DprE1-IN-1 DprE1-IN-1 is a potent inhibitor of DprE1 and PDE6.
T7954 YM976 YM976 is an orally active PDE4 inhibitor (IC50:2.2 nM)
T8405 Vardenafil hydrochloride Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes
TN1843 Kushenol K Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K ...
TN1950 Moracin M Moracin M is a phytoalexin. Moracin M inhibits PDE4D2, PDE4B2, PDE5A1, and PDE9A2 with the IC(50) values of 2.9, 4.5, >40, and >100 μM, respectively.
TN2095 Pomiferin Pomiferin is a natural product inhibitor of carbonic anhydrase I and II isoenzymes. It has anticancer, antibacterial and antidiabetic properties. Pomiferin has ...
TN1266 3-O-Methylquercetin 3-O-Methylquercetin is a selective and competitive PDE3/PDE4 inhibitor, and inhibits PDE3 than PDE4 with a low K(m) value; it inhibits total cAMP- and cGMP-phos...
TN2159 Robustine Robustine may have anti-inflammatory activity, it exhibits inhibition (IC 50 < or = 18.19 microM) of superoxide anion generation by human neutrophils in respons...
T12103 MR-L2 MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).
T12150 N-Methylbenzamide N-Methylbenzamide is a potent phosphodiesterase 10A (PDE10A) inhibitor,with anti-cancer activity.
T12315 OR-1896 OR-1896 is an active long-lived Levosimendan metabolite, is a highly selective inhibitor of phosphodiesterase (PDE) III isoformand a powerful vasodilator.
T12372 PAT-505 PAT-505 is a selective, noncompetitive and orally available inhibitor of autotaxin(IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma)...
T12394 PDE5-IN-2 PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5(IC50 of 0.31 nM)
T10994L Deltasonamide 2 hydrochloride Deltasonamide 2 hydrochloride is a competitive high-affinity PDEδ inhibitor with a Kd of approximately 385 pM.
T10994L2 Deltasonamide 2 (TFA) Deltasonamide 2 TFA is competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
T10994 Deltasonamide 2 Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
T8462 Enoximone Enoximone is a selective inhibitor of phosphodiesterase III (PDE3), with treatment of congestive heart failure.
T14352 Autotaxin-IN-1 Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship and it is used in trea...
T14507 Bay 60-7550 Bay 60-7550 is an inhibitor of PDE2(Ki: 3.8 nM).
T10481L BAY 73-6691 BAY 73-6691 is an inhibitor of brain penetrant PDE9A.
T10350 Apremilast D5 Apremilast D5 (CC-10004 D5) is a deuterium-labeled Apremilast. Apremilast is an orally available inhibitor of PDE-4 (IC50: 74 nM). Apremilast inhibits TNF-α re...
T10409 ATX inhibitor 5 ATX inhibitor 5 is an orally active autotaxin (ATX) inhibitor (IC50: 15.3 nM). It has an anti-hepatofibrosis effect and reduces CCl4-induced hepatic fibrosis le...
T10418 Autotaxin modulator 1 Autotaxin modulator 1 is a new modulator of Autotaxin extracted from Patent WO 2014018881 A1.
T10415 Autotaxin-IN-3 Autotaxin-IN-3 is an Autotaxin(ATX) inhibitor (IC50: 2.4 nM) sourced from patent WO2018212534A1 (compound 33).
T10416 Autotaxin-IN-4 Autotaxin-IN-4 is an Autotaxin inhibitor extracted from patent WO2018212534A1 (compound 51). It has the potential to treat idiopathic pulmonary fibrosis.
T10417 Autotaxin-IN-5 Autotaxin-IN-5 is an Autotaxin inhibitor extracted from patent WO2018212534A1 (compound 63). It has the potential to treat idiopathic pulmonary fibrosis.
T14962 CI-1044 CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).
T15381 Gisadenafil Gisadenafil is a specific and orally active inhibitor of PDE5 (IC50: 3.6 nM). It also prevents the degradation of cyclic guanosine monophosphate (cGMP).
T11206 ent-Tadalafil ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS).
T10730 CDC801 CDC801 is a potent and orally active inhibitor of PDE4 and TNF-α (IC50: 1.1 μM and 2.5 μM).
T11483 GSK 256066 Trifluoroacetate GSK 256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor (IC50: 3.2 pM for PDE4B). It can be used for the treatment of c...
T13193 TPN171 TPN171 is a selective and oral bioavailable phosphodiesterase type 5 (PDE5) inhibitor (IC50: 0.62 nM), which has the potential for the treatment of pulmonary ar...
T13232 TyK2-IN-2 TyK2-IN-2 is a selective inhibitor of TYK2 (IC50s: 7 nM, 0.1 μM, and 0.05 μM for TYK2 JH2, IL-23, and IFNα).
T10841 CM-675 CM-675 is a dual inhibitor of phosphodiesterase 5 (PDE5) and class I histone deacetylases (IC50s: 114 nM and 673 nM for PDE5 and HDAC1) with the potential to tr...
T15640 K134 K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
T15766 Lirimilast Lirimilast is an effective, selective, and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 49 nM). Lirimilast has potently anti-inflammatory propertie...
T16272 Naproxen etemesil Naproxen is a COX-1 and COX-2 inhibitor (IC50s: 8.72 and 5.15 μM, respectively in cell assay). Naproxen etemesil is a lipophilic and non-acidic prodrug of napr...
T5496 ML-030 ML-030 is a potent and selective inhibitor of PDE4(PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2 with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 4...
T16434 PAT-048 PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no e...
T16478 PF-04447943 PF-04447943 is an effective inhibitor of human recombinant PDE9A (IC50=12 nM). It has >78-fold selectivity, compared to other PDE family members (IC50>1000 nM).
T16482 PF-05085727 PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent...
T16484 PF-05180999 PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
T16498 Mardepodect hydrochloride Mardepodect hydrochloride can cross the blood-brain barrier. Mardepodect hydrochloride is an effective and selective PDE10A inhibitor (IC50: 0.37 nM). It has >1...
T16976 TAK-915 TAK-915 is a potent, selective, and brain-penetrant phosphodiesterase 2A (PDE2A) inhibitor (IC50: 0.61 nM). TAK-915 is >4100-fold more selectivity for PDE2A tha...
TN2974 3-O-Methylquercetin tetraacetate Quercetin 3-O-methyl ether is a potent phosphodiesterase (PDE)3/4 inhibitor, it has potential for treating asthma against ovalbumin-induced airway hyperresponsi...
TN4317 Isopedicin Isopedicin has anti-inflammatory functions, it inhibits the O(2)(*)(-) production in human neutrophils by an elevation of cellular cAMP and activation of PKA th...
TN4397 Kuraridine Kuraridine is measured against cGMP PDE5 to identify potent cGMP specific phosphodiesterase type 5 inhibitory constituents.
TN4665 Norbraylin Norbraylin is a natural product from Toddalia asiatica.
T8659 K-Ras-PDEδ-IN-1 K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ.It binds to the farnesyl binding pocket of PDEδ(Kd of 8 nM).
T8515 BI-409306 BI-409306 is a potent and selective inhibitor of PDE9A (IC50 of 52 nM),and can be used in the research of memory
T4462 Roflumilast N-oxide Roflumilast N-oxide is a PDE type 4 inhibitor.
T3465 Vesnarinone Vesnarinone (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal ne...
T21965 MBCQ MBCQ is an inhibitor of cGMP-specific phosphodiesterase PDE5.
T17199 Udenafil Udenafil is an inhibitor of PDE5 .
T16079 Mirodenafil Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.
T8787 Drotaverine hydrochloride Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation dur...
T8506 THPP-1 THPP-1 is a potent and orally bioavailable inhibitor of PDE10A(Ki of 1 nM and 1.3 nM for human and rat PDE10A, respectively).
T8454 SEP-0372814 SEP-0372814 is a potent inhibitor of PDE10.
T22086 HA-155 HA155 is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.
T2646 HA130 HA130 is a selective ATX (autotaxin) inhibitor.
T10410 ATX inhibitor 1 ATX inhibitor 1 is a potent ATX inhibitor (IC50: 1.23 nM, FS-3 and 2.18 nM, bis-pNPP).
T8919 Homo Sildenafil Homo Sildenafil is an analog of Sildenafil, It acts as a phosphodiesterase inhibitor.
Heptaminol hydrochloride
T0045CAS 543-15-7
Heptaminol hydrochloride, a vasoconstrictor, is used in the therapy of hypotension, especially orthostatic hypotension.
Pentoxifylline
T0070CAS 6493-05-6
Pentoxifylline modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase ...
Trapidil
T0080CAS 15421-84-8
Trapidil is a coronary vasodilator agent. It was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic...
Vardenafil
T0096CAS 224785-90-4
Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific...
Anagrelide
T0160CAS 68475-42-3
Anagrelide is a Platelet-reducing Agent. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by...
Vinpocetine
T0167CAS 42971-09-5
Vinpocetine is a selective inhibitor of cyclic GMP phosphodiesterase (PDE).
Zomepirac Sodium
T0264CAS 64092-48-4
Zomepirac sodium salt is a prostaglandin synthetase inhibitor.
Fenspiride hydrochloride
T0383CAS 5053-08-7
Fenspiride, an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of ...
Indometacin
T0458CAS 53-86-1
Indomethacin is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of indomethacin is as a Cyclooxygenase Inhibitor.
Cilostazol
T0462CAS 73963-72-1
Cilostazol is a Phosphodiesterase 3 Inhibitor. The mechanism of action of cilostazol is as a Phosphodiesterase 3 Inhibitor.
Sildenafil citrate
T0467CAS 171599-83-0
Sildenafil, a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less co...
Doxofylline
T0480CAS 69975-86-6
Doxofylline is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has show...
Theobromine
T0625CAS 83-67-0
3, 7-Dimethylxanthine, a xanthine alkaloid, is used as a bronchodilator and as a vasodilator.
Triflusal
T0705CAS 322-79-2
Triflusal is a 2-acetoxy-4-trifluoromethylbenzoic acid and it is an aspirin chemically-related molecule but not a derivative.
Diprophylline
T0892CAS 479-18-5
Dyphylline is a xanthine derivative. Dyphilline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Dyphilline prob...
Ketotifen fumarate
T0994CAS 34580-14-8
Ketotifen is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.
Roflumilast
T1024CAS 162401-32-3
Roflumilast is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activiti...
Luteolin
T1027CAS 491-70-3
Luteolin is a naturally occurring flavonoid. The flavonoids are polyphenolic compounds found as integral components of the human diet. In vitro work has concent...
Isoprenaline hydrochloride HOT
T1056CAS 51-30-9
Isoproterenol is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
Theophylline
T1083CAS 58-55-9
Theophylline is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant ac...
Theophylline monohydrate
T1083LCAS 5967-84-0
Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize ade...
Milrinone
T1096CAS 78415-72-2
Milrinone is a Phosphodiesterase 3 Inhibitor. The mechanism of action of milrinone is as a Phosphodiesterase 3 Inhibitor.
2-(Hydroxymethyl)pyridine
T1112CAS 586-98-1
2-Pyridinylmethanol is an organic compound.
Sildenafil
T1164CAS 139755-83-2
Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor, used to treat erectile dysfunction and reduce symptoms of pulmonary arterial hypertension (PAH).
Amrinone
T1265CAS 60719-84-8
Amrinone is a positive inotropic cardiotonic (cardiotonic agent) with vasodilator properties, phosphodiesterase 3 inhibitory activity.
Tadalafil
T1398CAS 171596-29-5
Tadalafil is a carboline-based compound with vasodilatory activity. Tadalafil selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 pho...
Dypyridamole
T1618CAS 58-32-2
Dipyridamole is a Platelet Aggregation Inhibitor. The physiologic effect of dipyridamole is by means of Decreased Platelet Aggregation.
Aminophylline
T1681CAS 317-34-0
Aminophylline is a competitive nonselective phosphodiesterase inhibitor giving a bronchodilatory effect.
Pimobendan
T1708CAS 74150-27-9
Pimobendan is a selective inhibitor of PDE3 (IC50: 0.32 μM).
IBMX HOT
T1713CAS 28822-58-4
IBMX is a pan-phosphodiesterase (PDE) inhibitor (IC50s: 6.5/26.3/31.7 μM for PDE3/PDE4/PDE5).
TAK063
T1745CAS 1238697-26-1
TAK-063 is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs.
Zaprinast
T2129CAS 37762-06-4
Zaprinast was an unsuccessful Clinicalal drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which succe...
Ibudilast
T2137CAS 50847-11-5
Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor. It is approved for use as an anti-inflammatory in Japan.
Theophylline-7-acetic acid
T2205CAS 652-37-9
Theophylline-7-acetic acid, a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in th...
Avanafil
T2334CAS 330784-47-9
Avanafil is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction.
Icariin
T2855CAS 489-32-7
Icariin is a flavonol glycoside, inhibiting PDE5 and PDE4 activities. Icariin also is a PPARα activator.
Apremilast
T2923CAS 608141-41-9
Apremilast (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.
PF8380
T3631CAS 1144035-53-9
PF-8380 is an effective and orally available autotaxin inhibitor (IC50: 2.8 nM, in isolated enzyme assay; 101 nM, in the human whole blood). It modulates lysoph...
Lotamilast
T3987CAS 947620-48-6
E6005 is a phosphodiesterase 4 (PDE-4) inhibitor (IC50: 2.8 nM) potentially for the treatment of atopic dermatitis.
GLPG1690
T4041CAS 1628260-79-6
GLPG-1690, an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.
Vardenafil hydrochloride trihydrate
T4097CAS 330808-88-3
Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
PF-2545920
T6042CAS 1292799-56-4
PF-2545920, a specific and effective PDE10A inhibitor (IC50=0.37 nM), is with more than1000-fold specificity activity over the PDE.
GSK256066
T6054CAS 801312-28-7
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380, 000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold sele...
Anagrelide HCl
T6390CAS 58579-51-4
Anagrelide Hydrochloride(BL4162A) is a drug used for the treatment of essential thrombocytosis.
Cilomilast
T6445CAS 153259-65-5
Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.
Deltarasin
T6462CAS 1440898-61-2
Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Irsogladine
T6548CAS 57381-26-7
Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
Rolipram
T6644CAS 61413-54-5
Rolipram is a phosphodiesterase 4 inhibitor with antidepressant properties.
S- (+)-Rolipram
T6649CAS 85416-73-5
S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous...
Sildenafil Mesylate
T6983CAS 1308285-21-3
Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
Crisaborole
T4285CAS 906673-24-3
AN-2728 is a Phosphodiesterase 4 Inhibitor.
(+)-pinoresinol-β-D-glucoside; (+)-pinor
T4S0792CAS 69251-96-3
CP671305
T4695CAS 445295-04-5
CP671305 is an orally active, potent and selective inhibitor of phosphodiesterase-4-D.
BRL 50481
T5106CAS 433695-36-4
BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.
Olprinone
T5033CAS 106730-54-5
Olprinone(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor.Olprinone has been reported to improve microcirculation and attenuate inflammation. Olp...
BW-A78U
T5101CAS 101155-02-6
BW-A 78U is a PDE4 inhibitor (IC50: 3 μM). It is not inhibition on the lipopolysaccharide (LPS)-induced TNF-α release.
Ginkgolide J
T6S2115CAS 107438-79-9
Ginkgolide J has neuroprotective activity, it can prevent A beta(1-42) induced inhibition of long-term potentiation in the CA1 region of mouse hippocampal slice...
SEP-0372814
T5411CAS 1516896-09-5
PDE10-IN-1 is PDE10-IN-1 inhibitor extracted from Patent WO 2013192273 A1, for treating CNS and metabolic disorders.
D 159687
T5474CAS 1155877-97-6
D159687 is a selective PDE4D inhibitor,had a procognitive profile as it improved memory in the novel object recognition test but had no antidepressant or anxi...
VP3.15 dihydrobromide
T5956CAS 1281681-33-1
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE7- glycogen synthase kinase (GSK)3 inhibitor(with IC50s of 1...
Nortadalafil
T6147CAS 171596-36-4
Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, treating erectile dysfunction (ED) ; and under the name Adcirca for the treatment of pulmonary ar...
Proxyphylline
T5940CAS 603-00-9
Proxyphylline is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and...
Lodenafil
T7346CAS 139755-85-4
Lodenafil is a potent PDE5 inhibitor, with treatment of erectile dysfunction (ED)
Amino Tadalafil
T7542CAS 385769-84-6
Amino tadalafil is a potent phosphodiesterase 5 (PDE5) inhibitor.
Cilostamide
T7642CAS 68550-75-4
Cilostamide is a selective phosphodiesterase (PDE)3A and PDE3B inhibitor(IC50 values of 27 and 50 nM, respectively)
Mirodenafil dihydrochloride
TQ0126CAS 862189-96-6
Mirodenafil (SK3530) dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.
DprE1-IN-1
T3224CAS 1494675-86-3
DprE1-IN-1 is a potent inhibitor of DprE1 and PDE6.
YM976
T7954CAS 191219-80-4
YM976 is an orally active PDE4 inhibitor (IC50:2.2 nM)
Vardenafil hydrochloride
T8405CAS 224785-91-5
Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes
Kushenol K
TN1843CAS 101236-49-1
Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K ...
Moracin M
TN1950CAS 56317-21-6
Moracin M is a phytoalexin. Moracin M inhibits PDE4D2, PDE4B2, PDE5A1, and PDE9A2 with the IC(50) values of 2.9, 4.5, >40, and >100 μM, respectively.
Pomiferin
TN2095CAS 572-03-2
Pomiferin is a natural product inhibitor of carbonic anhydrase I and II isoenzymes. It has anticancer, antibacterial and antidiabetic properties. Pomiferin has ...
3-O-Methylquercetin
TN1266CAS 1486-70-0
3-O-Methylquercetin is a selective and competitive PDE3/PDE4 inhibitor, and inhibits PDE3 than PDE4 with a low K(m) value; it inhibits total cAMP- and cGMP-phos...
Robustine
TN2159CAS 2255-50-7
Robustine may have anti-inflammatory activity, it exhibits inhibition (IC 50 < or = 18.19 microM) of superoxide anion generation by human neutrophils in respons...
MR-L2
T12103CAS 2374703-19-0
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).
N-Methylbenzamide
T12150CAS 613-93-4
N-Methylbenzamide is a potent phosphodiesterase 10A (PDE10A) inhibitor,with anti-cancer activity.
OR-1896
T12315CAS 220246-81-1
OR-1896 is an active long-lived Levosimendan metabolite, is a highly selective inhibitor of phosphodiesterase (PDE) III isoformand a powerful vasodilator.
PAT-505
T12372CAS 1782070-22-7
PAT-505 is a selective, noncompetitive and orally available inhibitor of autotaxin(IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma)...
PDE5-IN-2
T12394CAS 2244517-61-9
PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5(IC50 of 0.31 nM)
Deltasonamide 2 hydrochloride
T10994LCAS T10994L
Deltasonamide 2 hydrochloride is a competitive high-affinity PDEδ inhibitor with a Kd of approximately 385 pM.
Deltasonamide 2 (TFA)
T10994L2CAS 2235358-74-2
Deltasonamide 2 TFA is competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
Deltasonamide 2
T10994CAS 2088485-34-9
Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
Enoximone
T8462CAS 77671-31-9
Enoximone is a selective inhibitor of phosphodiesterase III (PDE3), with treatment of congestive heart failure.
Autotaxin-IN-1
T14352CAS 1619971-30-0
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship and it is used in trea...
Bay 60-7550
T14507CAS 439083-90-6
Bay 60-7550 is an inhibitor of PDE2(Ki: 3.8 nM).
BAY 73-6691
T10481LCAS 794568-92-6
BAY 73-6691 is an inhibitor of brain penetrant PDE9A.
Apremilast D5
T10350CAS 1258597-47-5
Apremilast D5 (CC-10004 D5) is a deuterium-labeled Apremilast. Apremilast is an orally available inhibitor of PDE-4 (IC50: 74 nM). Apremilast inhibits TNF-α re...
ATX inhibitor 5
T10409CAS 2402772-45-4
ATX inhibitor 5 is an orally active autotaxin (ATX) inhibitor (IC50: 15.3 nM). It has an anti-hepatofibrosis effect and reduces CCl4-induced hepatic fibrosis le...
Autotaxin modulator 1
T10418CAS 1548743-69-6
Autotaxin modulator 1 is a new modulator of Autotaxin extracted from Patent WO 2014018881 A1.
Autotaxin-IN-3
T10415CAS 2156655-68-2
Autotaxin-IN-3 is an Autotaxin(ATX) inhibitor (IC50: 2.4 nM) sourced from patent WO2018212534A1 (compound 33).
Autotaxin-IN-4
T10416CAS 2156655-86-4
Autotaxin-IN-4 is an Autotaxin inhibitor extracted from patent WO2018212534A1 (compound 51). It has the potential to treat idiopathic pulmonary fibrosis.
Autotaxin-IN-5
T10417CAS 2156655-99-9
Autotaxin-IN-5 is an Autotaxin inhibitor extracted from patent WO2018212534A1 (compound 63). It has the potential to treat idiopathic pulmonary fibrosis.
CI-1044
T14962CAS 197894-84-1
CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).
Gisadenafil
T15381CAS 334826-98-1
Gisadenafil is a specific and orally active inhibitor of PDE5 (IC50: 3.6 nM). It also prevents the degradation of cyclic guanosine monophosphate (cGMP).
ent-Tadalafil
T11206CAS 629652-72-8
ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS).
CDC801
T10730CAS 192819-27-5
CDC801 is a potent and orally active inhibitor of PDE4 and TNF-α (IC50: 1.1 μM and 2.5 μM).
GSK 256066 Trifluoroacetate
T11483CAS 1415560-64-3
GSK 256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor (IC50: 3.2 pM for PDE4B). It can be used for the treatment of c...
TPN171
T13193CAS 1229018-87-4
TPN171 is a selective and oral bioavailable phosphodiesterase type 5 (PDE5) inhibitor (IC50: 0.62 nM), which has the potential for the treatment of pulmonary ar...
TyK2-IN-2
T13232CAS 2098466-94-3
TyK2-IN-2 is a selective inhibitor of TYK2 (IC50s: 7 nM, 0.1 μM, and 0.05 μM for TYK2 JH2, IL-23, and IFNα).
CM-675
T10841CAS 1872466-47-1
CM-675 is a dual inhibitor of phosphodiesterase 5 (PDE5) and class I histone deacetylases (IC50s: 114 nM and 673 nM for PDE5 and HDAC1) with the potential to tr...
K134
T15640CAS 189362-06-9
K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
Lirimilast
T15766CAS 329306-27-6
Lirimilast is an effective, selective, and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 49 nM). Lirimilast has potently anti-inflammatory propertie...
Naproxen etemesil
T16272CAS 385800-16-8
Naproxen is a COX-1 and COX-2 inhibitor (IC50s: 8.72 and 5.15 μM, respectively in cell assay). Naproxen etemesil is a lipophilic and non-acidic prodrug of napr...
ML-030
T5496CAS 1013750-77-0
ML-030 is a potent and selective inhibitor of PDE4(PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2 with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 4...
PAT-048
T16434CAS 1359983-15-5
PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no e...
PF-04447943
T16478CAS 1082744-20-4
PF-04447943 is an effective inhibitor of human recombinant PDE9A (IC50=12 nM). It has >78-fold selectivity, compared to other PDE family members (IC50>1000 nM).
PF-05085727
T16482CAS 1415637-72-7
PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent...
PF-05180999
T16484CAS 1394033-54-5
PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
Mardepodect hydrochloride
T16498CAS T16498
Mardepodect hydrochloride can cross the blood-brain barrier. Mardepodect hydrochloride is an effective and selective PDE10A inhibitor (IC50: 0.37 nM). It has >1...
TAK-915
T16976CAS 1476727-50-0
TAK-915 is a potent, selective, and brain-penetrant phosphodiesterase 2A (PDE2A) inhibitor (IC50: 0.61 nM). TAK-915 is >4100-fold more selectivity for PDE2A tha...
3-O-Methylquercetin tetraacetate
TN2974CAS 1486-69-7
Quercetin 3-O-methyl ether is a potent phosphodiesterase (PDE)3/4 inhibitor, it has potential for treating asthma against ovalbumin-induced airway hyperresponsi...
Isopedicin
TN4317CAS 4431-42-9
Isopedicin has anti-inflammatory functions, it inhibits the O(2)(*)(-) production in human neutrophils by an elevation of cellular cAMP and activation of PKA th...
Kuraridine
TN4397CAS 34981-25-4
Kuraridine is measured against cGMP PDE5 to identify potent cGMP specific phosphodiesterase type 5 inhibitory constituents.
Norbraylin
TN4665CAS 60796-64-7
Norbraylin is a natural product from Toddalia asiatica.
K-Ras-PDEδ-IN-1
T8659CAS 1841464-21-8
K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ.It binds to the farnesyl binding pocket of PDEδ(Kd of 8 nM).
BI-409306
T8515CAS 1189767-28-9
BI-409306 is a potent and selective inhibitor of PDE9A (IC50 of 52 nM),and can be used in the research of memory
Roflumilast N-oxide
T4462CAS 292135-78-5
Roflumilast N-oxide is a PDE type 4 inhibitor.
Vesnarinone
T3465CAS 81840-15-5
Vesnarinone (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal ne...
MBCQ
T21965CAS 150450-53-6
MBCQ is an inhibitor of cGMP-specific phosphodiesterase PDE5.
Udenafil
T17199CAS 268203-93-6
Udenafil is an inhibitor of PDE5 .
Mirodenafil
T16079CAS 862189-95-5
Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.
Drotaverine hydrochloride
T8787CAS 985-12-6
Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation dur...
THPP-1
T8506CAS 1257051-63-0
THPP-1 is a potent and orally bioavailable inhibitor of PDE10A(Ki of 1 nM and 1.3 nM for human and rat PDE10A, respectively).
SEP-0372814
T8454CAS 1516895-53-6
SEP-0372814 is a potent inhibitor of PDE10.
HA-155
T22086CAS 1229652-22-5
HA155 is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.
HA130
T2646CAS 1229652-21-4
HA130 is a selective ATX (autotaxin) inhibitor.
ATX inhibitor 1
T10410CAS 2225892-70-4
ATX inhibitor 1 is a potent ATX inhibitor (IC50: 1.23 nM, FS-3 and 2.18 nM, bis-pNPP).
Homo Sildenafil
T8919CAS 642928-07-2
Homo Sildenafil is an analog of Sildenafil, It acts as a phosphodiesterase inhibitor.