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.