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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.

Bucladesine sodium
T141816980-89-5
Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.
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IBMX
T171328822-58-4
IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5 26.3 31.7 μM). IBMX enhances the intracellular cAMP level.
  • $26.4
  • $33
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Luteolin
T1027491-70-3
Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.
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BI 1015550
T720311423719-30-5
Nerandomilast (BI 1015550) is an orally active PDE4B inhibitor with IC50 of 7.2 nM. BI 1015550 has potential applications in inflammation, allergic diseases, pulmonary fibrosis and chronic obstructive pulmonary disease (COPD) with a good safety profile.
  • $59
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MR-L2
T121032374703-19-0
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).
  • $148
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Gisadenafil
T15381334826-98-1In house
Gisadenafil (UK-369003), a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM, prevents the degradation of cGMP.
  • $195
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PF-04822163
T283671798334-07-2In house
PF-04822163 is a potent inhibitor of PDE1 with IC50 value of 0.0024 μM.
  • $350
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Isoprenaline hydrochloride
T105651-30-9
Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
  • $33
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Tanimilast
T386251239278-59-1In house
Tanimilast (CHF-6001) is a novel, potent, and selective phosphodiesterase 4 inhibitor with an IC50 value of 0.026 ± 0.006 nM. It exhibits potent anti-inflammatory activity and is indicated for topical use in the lungs. Tanimilast was studied for its effects on obstructive lung disease.
  • $233
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Pumafentrine
T71691207993-12-2In house
Pumafentrine(BY 343) is a dual PDE3 PDE4 inhibitor that reduces clinical scores and TNF expression in experimental colitis in mice.
  • $195
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Roflumilast N-oxide
T4462292135-78-5
Roflumilast N-oxide is an inhibitor of PDE type 4.
  • $30
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Roflumilast
T1024162401-32-3
Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.
  • $50
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TPN171
T131931229018-87-4In house
TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.
  • $133
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PF-07038124 HCl
T60921L2415317-57-4In house
PF-07038124 HCl is a selective and potent PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2.PF-07038124 HCl inhibits IL-13, IL-4, and IFNγ, and can be used in the study of skin disorders such as atopic dermatitis and plaque psoriasis.
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AWD 12-281
T30232257892-33-4In house
AWD 12-281 is a selective phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory and bronchodilator activity used in the study of chronic obstructive pulmonary disease (COPD).
  • $293 TargetMol
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PF-04957325
T124221305115-80-3
PF-04957325 is a potent and selective inhibitor of PDE8.PF-04957325 has an IC50 of 0.7 nM for PDE8A and 0.3 nM for PDE8B.PF-04957325 can be used to study autoimmune encephalomyelitis.
  • $139
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Icariin
T2855489-32-7
Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432 73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.
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Zaprinast
T212937762-06-4
Zaprinast is a cGMP-selective phosphodiesterase (PDE) inhibitor and a GPR35 agonist. It has a strong activating effect on rat GPR35 and a certain activating effect on human GPR35. It reduces vascular remodeling through anti-proliferative and pro-apoptotic effects.
  • $32
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Difamilast
T27172937782-05-3
Difamilast is an inhibitor of phosphodiesterase IV.
  • $63
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ITI-214
T116891642303-38-5
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  • $68
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UK 227786
T11220L150452-21-4In house
UK 227786 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.
  • $117
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Parogrelil Free Base
T70793139145-27-0In house
Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.
  • $293
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Cudetaxestat
T631901782070-21-6
Cudetaxestat (BLD-0409) is a potent, orally active autotaxin inhibitor.
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Tadalafil
T1398171596-29-5
Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.
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Rolipram
T664461413-54-5
Rolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.
  • $43
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Levosimendan
T2530141505-33-1
Levosimendan (OR1259) is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner.
  • $31
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Drotaverine hydrochloride
T8787985-12-6
Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation during childbirth. Drotaverine hydrochloride is structurally related to papaverine
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Sildenafil citrate
T0467171599-83-0
Sildenafil citrate (UK-92480 citrate) , a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less commonly for pulmonary hypertension.
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Nortadalafil
T6147171596-36-4
Nortadalafil (Demethyl Tadalafil) is demethyl Tadalafil, which is a PDE5 inhibitor, treating erectile dysfunction (ED) ; and under the name Adcirca for the treatment of pulmonary arterial hypertensio.
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Dovramilast
T63056340019-69-4In house
Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor that reduces the production of pro-inflammatory mediators and cytokines. Dovramilast is used in the study of Mycobacterium tuberculosis infections and lupus erythematosus.
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Indomethacin
T045853-86-1
Indomethacin (Indomethacin) is a COX1 and COX2 inhibitor (IC50=18 26 nM) with blood-brain barrier permeability and non-selectivity. Indomethacin is a non-steroidal anti-inflammatory agent with anti-tumor and anti-infective activity.
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Theophylline monohydrate
T1083L5967-84-0
Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.
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Butein
T6427487-52-5
Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.
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Torbafylline
T67965105102-21-4In house
Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.
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Nauclefine
TN612057103-51-2
Nauclefine (Parvine) is a plant indole alkaloid natural product and induces apoptosis of diverse cancer cells via a PDE3A-SLFN12 dependent death pathway. Nauclefine binds PDE3A but does not inhibit the PDE3A's phosphodiesterase activity.
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Enpp-1-IN-14
T601052687222-59-7
Enpp-1-IN-14 is a potent inhibitor of Ectonucleotide Pyrophosphatase Phosphodiesterase-1 (ENPP1) with an IC50 value of 32.38 nM for recombinant human ENPP-1. Enpp-1-IN-14 has anti-tumor activity.
  • $51
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Apremilast
T2923608141-41-9
Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.
  • $43
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TP-10
T13189898563-00-3
TP-10 is a selective inhibitor of PDE10A against other PDEs with IC50 of 0.8 nM.
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CALP2 acetate(261969-04-4 free base)
TP1909L1
CALP2 acetate is an antagonist of calmodulin showing high affinity for binding to the CaM EF-hand/Ca2+-binding site with a Kd of 7.9 µM. CALP2 acetate potently inhibits of adhesion and degranulation. CALP2 acetate is also a strong activator of alveolar macrophages. CALP2 acetate inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations.
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Crisaborole
T4285906673-24-3
Crisaborole (AN-2728) is a phosphodiesterase 4 inhibitor.
  • $38
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Carbazeran
T2145770724-25-3
Carbazeran (UK-31,557) is an inhibitor of PDE2 and PDE3 and can be used for studies about metabolic diseases. Carbazeran shows inotropic and chronotropic effects in vivo(EC50 = 100 μM).
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Triflusal
T0705322-79-2
Triflusal (UR1501) is a 2-acetoxy-4-trifluoromethylbenzoic acid and it is an aspirin chemically-related molecule but not a derivative.
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CP 461
T31020227619-96-7In house
CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.
  • $195
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Pimobendan
T170874150-27-9
Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 (IC50: 0.32 μM).
  • $32
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ENPP1 Inhibitor C
T374312378640-92-5
ENPP1 Inhibitor C is an ectonucleotide pyrophosphatase phosphodiesterase 1 (ENPP1) inhibitor with potential anticancer activity for the study of triple-negative breast cancer.
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    CDC801
    T10730192819-27-5
    CDC801 is an inhibitor of PDE4 and TNF-α with IC50s of 1.1 μM and 2.5 μM, respectively.
    • $173
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    Mopidamol
    T2582913665-88-8In house
    Mopidamol (RA 233) is a phosphodiesterase inhibitor, a dipyridamole derivative, with anticancer activity that prevents retinal vascular defects in experimental diabetes.
    • $380
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    Robustine
    TN21592255-50-7
    Robustine is a natural product, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro.
    • $73
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