Home > Inhibitors & Agonists > Metabolic Enzyme/Protease > Phosphodiesterase (PDE)
Cat. No. Product name CAS No.
DC9584 (R)-(-)-Rolipram

(R)-(-)-Rolipram is a potent and cAMP-specific PDE4 inhibitor with IC50 of 0.22 uM; 2.5-fold more potent than (+)-rolipram (IC50= 2.58 uM) in inhibiting membrane-bound PDE 4.

85416-75-7
DC9581 (S)-(+)-Rolipram

(S)-(+)-Rolipram is a PDE4-inhibitor and an anti-inflammatory agent, less potent than its R enantiomer.

85416-73-5
DC11936 TAK-915

A highly potent, selective, brain-penetrating and orally active phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 0.61 nM.

1476727-50-0
DC11663 GS-5759

A novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).

1346653-91-5
DC11559 PDE5-IN-6c

A novel potent, selective PDE5 inhibitor with IC50 of 0.056 nM for PDE5A1.

1448419-13-3
DC11969 (S)-C33

A novel potent, selective PDE9A inhibitor with IC50 of 11 nM, >45-fold selectivity over other PDE isoforms.

2066488-39-7
DC11777 PDM-631

A novel potent, selective, brain-penetrable and orally active PDE2A inhibitor with IC50 of 1.5 and 4.2 nM for human and rat PDE2A, respectively.

2095312-08-4
DC11660 PF-4181366

A potent, selective, brain penetrant PDE9A inhibitor with IC50 of 1.8 nM.

1082743-32-5
DC12002 AMG 580

AMG 580 (AMG580) is a novel potent, selective phosphodiesterase 10A (PDE10A) inhibitor with IC50 of 0.13 nM.

1227067-71-1
DC11878 AMG-579

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM.

1227067-61-9
DC7815 Crisaborole(AN-2728) Featured

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

906673-24-3
DC7063 Apremilast Featured

Apremilast(CC10004) is a novel small molecule inhibitor of PDE4 with an IC50 value of 74 nM.

608141-41-9
DC8799 Avanafil(TA-1790) Featured

Avanafil(TA-1790) is a potent and highly selective phosphodiesterase-5(PDE-5) inhibitor(IC50=5.2 nM) for erectile dysfunction; lower selectivity against PDE1, PDE6, and PDE11.

330784-47-9
DC9578 Bay 60-7550 Featured

Bay 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human); 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5, PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A.

439083-90-6
DC11389 BI 409306 Featured

BI 409306 is an inhibitor of phosphodisterase 9A(PDE9A).

1189767-28-9
DC12041 BW-A 78U Featured

BW-A 78U is a PDE4 inhibitor with an IC50 of 3 μM.

101155-02-6
DCAPI1569 Cilostazol

Cilastazol is a 2-oxo-quinoline with vasodilator, antimitogenic, antithrombotic, and cardiotonic properties. This compound has been shown to cause inhibition of adenosine uptake, eventually resulting in changes to cAMP levels. Studies have shown Cilostazo

73963-72-1
DC9582 Cilomilast

Cilomilast(SB 207499; Ariflo) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity.

153259-65-5
DC8205 Deltarasin Featured

Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.

1440898-61-2
DC10141 E6005 Featured

E6005 potently and selectively inhibited human PDE4 activity with an IC50 of 2.8 nM and suppressed the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM.

947620-48-6
DC8767 GSK256066 Featured

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 selectivity against PDE4B versus PDE7.

801312-28-7
DC7676 IBMX(NSC165960; SC2964) Featured

IBMX(NSC165960; SC2964) is a competitive nonselective PDEs inhibitor with IC50 of 2-50 uM but does not inhibit PDE8 or PDE9; nonselective adenosine receptor antagonist.

28822-58-4
DCAPI1578 Irsogladine maleate

Irsogladine maleate is a selective PDE4 inhibitor that facilitates gap junction intercellular communication through muscarinic acetylcholine receptor binding. It is a potent inhibitor of angiogenesis in wild-type and plasminogen activator-deficient mice.

84504-69-8
DC3158 Milrinone Featured

Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE

78415-72-2
DC9579 Nortadalafil Featured

Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension. IC50 value: Ta

171596-36-4
DC9583 Oglemilast

Oglemilast(GRC3886) is a potent PDE4 inhibitor, under clinical studies in the treatment of allergen-induced asthma.

778576-62-8
DC9577 Olprinone (Hydrochloride) Featured

Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor.

119615-63-3
DC10345 PDE1-IN-2

PDE1-IN-2 is an inhibitor of PDE1 extracted from patent WO2016/55618 A1, example 31; has IC50 values of 6, 140 and 164 nM for PDE1C, PDE1B and PDE1A, respectvely.

1904611-63-7
DC11367 PF-04447943 Featured

PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.

1082744-20-4
DC10418 PF-04957325

PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50 values of 0.7 nM for PDE8A and less than 0.3 nM for PDE8B.

1305115-80-3
DC11937 PF 05180999 Featured

PF-05180999 (PF 5180999) is a potent, selective, brain-penetrating and orally bioavailable phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 1 nM.

1394033-54-5
DC7201 PF-2545920(MP-10) Featured

PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM.

898562-94-2
DC7247 PF-8380 Featured

PF-8380 is a potent and specofic autotaxin inhibitor with an IC50 value of 2.8 nM.

1144035-53-9
DC4146 Roflumilast Featured

Roflumilast (Daxas) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.

162401-32-3
DC11671 RPL-554

RPL-554 (LS-193855, RPL554) is a potent, orally available, dual PDE3/PDE4 inhibitor with IC50 of 0.4 nM and 1479 nM, respectively.

298680-25-8
DC8048 SEP-0372814 Featured

SEP-0372814 is a potent PDE10 inhibitor.

1516895-53-6
DC9779 Sildenafil citrate Featured

Sildenafil citrate, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.

171599-83-0
DC7298 MY-5445

Specific inhibitor of cyclic GMP phosphodiesterase, selective for PDE5 (IC50 = 0.5 μM).

78351-75-4
DC5901 Tadalafil Featured

Tadalafil is a potent and selective inhibitor of Phosphodiesterase-5 (PDE5) This compound prevents the breakdown of phosphodiesterases, many of which are used as secondary messengers. By preventing the breakdown of these messenger molecules, tadalafil can

171596-29-5
DC7945 TAK-063 Featured

TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.

1238697-26-1
DC11661 BAY 73-6691

BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype.

794568-92-6
DC4133 Udenafil

Udenafil is a new phosphodiesterase type 5 (PDE5) inhibitor used to treat erectile dysfunction (ED)

268203-93-6
DC9182 Vardenafil hydrochloride trihydrate Featured

Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.

330808-88-3
DC9847 Vesnarinone(OPC8212) Featured

Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.

81840-15-5
DC28354 (E/Z)HA-155 Featured

(E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.

1229652-22-5
DC28378 THPP-1 Featured

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.

1257051-63-0
DC28708 ATX inhibitor 5

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 has anti-hepatofibrosis effect, and reduces CCl4-induced hepatic fibrosis level prominently.

2402772-45-4
DC28759 Autotaxin-IN-3

Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with an IC50 of 2.4 nM, compound 33, sourced from patent WO2018212534A1.

2156655-68-2
DC28761 Autotaxin-IN-4

Autotaxin-IN-4 (compound 51), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat idiopathic pulmonary fibrosis.

2156655-86-4
DC28762 Autotaxin-IN-5

Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis.

2156655-99-9
DC29002 Siguazodan

Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.

115344-47-3
DC29034 ent-Tadalafil

ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM.

629652-72-8
DC40058 GSK356278

GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.

720704-34-7
DC40284 Kuraridine

Kuraridine is a prenylated flavonol extract from the roots of?Sophora flavescens. Kuraridine an inhibitory effect on cGMP specific phosphodiesterase type 5?(PDE5) and has an IC50 of 0.64 μM.

34981-25-4
DC40378 MR-L2 Featured

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM.

2374703-19-0
DC40484 Homo Sildenafil

Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor.

642928-07-2
DC40895 BRD9500

BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.

1630760-75-6
DC40977 DSR-141562 Featured

DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.

2007975-22-4
DC41053 Acetildenafil

Acetildenafil is a derivative of the phosphodiesterase 5 (PDE5) inhibitor Sildenafil.

831217-01-7
DC41313 3-O-Methylquercetin

3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values of 31.9 μM, 86.9 μM, 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively.

1486-70-0
DC41342 Ayanin

Ayanin is a bioflavonoid isolated from Croton schiedeanus Schlecht. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al.

572-32-7
DC41379 Ilexsaponin B2

Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively.

108906-69-0
DC41489 Kushenol B

Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities. Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 μM.

99217-64-8
DC42340 Autotaxin modulator 1

Autotaxin modulator 1 is an autotaxin (ATX) enzyme, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer.

1548743-69-6
DC42341 LY-411575 (isomer 3)

LY-411575 isomer 3 is an isomer of LY411575, which is a potent γ-secretase.

DC42521 MBCQ Featured

MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.

150450-53-6
DC44761 Vardenafil hydrochloride

Vardenafil (BAY38-9456, Levitra, Staxyn) hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase (PDE) with IC50 of 0.7 nM, 11 nM and 180 nM for PDE5, PDE6 and PDE1, respectively.

224785-91-5
DC45449 (+)-Medioresinol Di-O-β-D-glucopyranoside

(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitory activity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase.

88142-63-6
DC46127 Sildenafil-d3

Sildenafil-d3 is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

1126745-90-1
DC46173 FR-229934

FR-229934 is a PDE V inhibitor extracted from patent WO2019130052A1. FR-229934 can be used for the research of pulmonary arterial hypertension and erectile dysfunction.

799841-02-4
DC46253 LASSBio-1632

LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.

DC46402 Tovinontrine

Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.

2062661-53-2
DC46435 PF-8380 hydrochloride

PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.

DC46873 Senazodan hydrochloride

Senazodan (MCI 154) (hydrochloride), as a Ca2+ sensitiser, shows inhibition effect on PDE III.

98326-33-1
DC46874 Carbazeran citrate

Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease.

153473-94-0
DC47087 Orismilast

Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases.

1353546-86-7
DC47201 Irsenontrine

Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE 9) inhibitor. Irsenontrine can be used for the research of neurological diseases.

1429509-82-9
DC47223 Ro 20-1724

Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect.

29925-17-5
DC47386 N-Desmethyl Sildenafil

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

139755-82-1
DC47387 PDE4-IN-3

PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).

DC47882 TMX-4113

TMX-4113 is a degrader of phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). TMX-4113 can be used for the research of cancer.

DC47883 TMX-4100

TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma.

2367619-63-2
DC47925 PDE4-IN-4

PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled treatment of pulmonary diseases.

1793069-00-7
DC47989 FPFT-2216 Featured

FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.

2367619-87-0
DC48220 Mufemilast

Mufemilast is a phosphodiesterase 4 (PDE4) inhibitor.

1255909-03-5
DC48221 Andolast

Andolast is an anti-allergic agent for the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD). Andolast inhibits dose dependently guinea-pig lung cAMP-phosphodiesterase with an IC50 of 50 mM.

132640-22-3
DC48222 Arofylline

Arofylline is a PDE4 inhibitor as a potential treatment for asthma.

136145-07-8
DC48223 ATX inhibitor 7

ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.

1646784-47-5
DC48224 Cudetaxestat

Cudetaxestat (BLD-0409) is a potent and orally active autotaxin (ATX) inhibitor.

1782070-21-6
DC48225 PDE2A-IN-1

PDE2A-IN-1 is a phosphodiesterase 2A (PDE2A) inhibitor with an IC50 value of 1.3 nM.

2648290-28-0
DC48226 ONO-8430506 Featured

ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.

1354805-08-5
DC48693 Enpp-1-IN-9

Enpp-1-IN-9 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-9 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).

2718970-70-6
DC48696 Enpp-1-IN-5

Enpp-1-IN-5 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-5 has the potential for the research of cancer and infectious diseases (extracted from patent WO2019046778A1/WO2021203772A1, compound 1).

2230916-95-5
DC48714 Enpp-1-IN-7

Enpp-1-IN-7 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-7 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).

DC48745 Enpp-1-IN-4

Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1).

2376600-89-2
DC48763 Enpp-1-IN-8

Enpp-1-IN-8 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-8 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).

2718971-08-3
DC48871 Enpp-1-IN-6

Enpp-1-IN-6 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-6 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).

2718971-29-8
DC48927 Hcyb1

Hcyb1 is a highly selective PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling.

DC48957 Drotaverine hydrochloride

Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.

985-12-6
DC49054 ATX inhibitor 8

ATX inhibitor 8 is a Autotaxin (ATX) inhibitor extracted from patent WO2018212534A1 compound 96.

2156656-37-8
DC49125 Toddacoumalone

Toddacoumalone is a natural inhibitor of phosphodiesterase 4 (PDE4) with moderate potency and imperfect drug-like properties. Toddacoumalone has the potential for the research of inflammatory diseases such as psoriasis.

139750-79-1
DC49744 PDE4-IN-5

PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect.

DC49746 PF-07038124

PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1 1.06 nM, respectively).

2415085-44-6
DC49747 PDE4-IN-8

PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM).

2415085-45-7
DC70144 GSK-256066

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/23/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.

1415560-64-3
DC70165 AA6216

AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.AA6216 showed stronger inhibitory effects against PDE4 than other PDE family members. AA6216 potently inhibits cytokine production (TNF-α,IL-12p40, IL-4, and IL-13, IC50s=2.2-7.9 nM) by PBMCs stimulated with PHA.AA6216 inhibited the production of TGF-β1 by a human monocytic cell line THP-1, AA6216 dose-dependently reduced the production of TNF-α by alveolar macrophages from patients with IPF.AA6216 demonstrated anti-fibrotic potency on mouse model of bleomycin-induced lung fibrosis.

1644280-85-2
DC70239 BAY 2666605 Featured

BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis.

2275774-60-0
DC70277 BVQ1814

BVQ1814 (BVQ-1814) is a highly effective fluorescent probe targeting PDE10A with highly potent affinity (IC50=0.9 nM), >1000-fold subfamily selectivity.

DC70322 CPL500036

CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation.

1829530-11-1
DC70576 LY2775240

LY2775240 (LY-2775240) is a highly selective, potent and orally active inhibitor of phosphodiesterase 4 (PDE4) with IC50 of 0.09/0.09/2.4/0.14 nM for PDE4A/B/C/D.LY2775240 displays >200-fold selectivity over PDE10A, and >5000-fold selectivity over other PDE isoforms (IC50>10 uM).LY2775240 potently inhibits TNFα secreted induced by Toll‐like receptor 4 agonist LPS in a human whole blood assay, inhibited LPS‐stimulated TNFα but has no effect with the media‐only control.LY2775240 is more potent than apremilast (IC50, 18 nM vs. 290 nM), also affects E‐selectin, secreted IgG, plasminogen activator inhibitor‐1, and secreted IL‐10.

1628160-15-5
DC70683 PF-04827736

PF-04827736 ((S)-PF-04677490) is a potent, selective PDE1 inhibitor with IC50 of 42, 9.1 and 38 nM for PDE1A, PDE1B and PDE1C, respectively; displays >10-fold selectivity over PDE10A1, and >45-fold selectivity over other PDE isoforms.

DC71151 T-0156

T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.

324572-93-2
DC71384 Roflupram

Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors.

1093412-18-0
DC71385 NPD-001

NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM.

469863-16-9
DC71683 Lodenafil Featured

Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).

139755-85-4
DC71812 Avanafil dibenzenesulfonate

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

330784-48-0
DC72219 Ambuphylline

Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases.

5634-34-4
DC72220 (R)-Irsenontrine

(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine, is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases.

1429509-81-8
DC72221 Phenacaine

Phenacaine (Holocaine) is a local anesthetic. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase and cyclic nucleotide phosphodiesterases from brain and heart.

101-93-9
DC72376 PF-03049423 free base

PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke.

954138-07-9
DC72377 Deltasonamide 1 TFA

Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors.

2235358-73-1
DC72668 Etazolate hydrochloride

Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.

35838-58-5
DC72669 PAT-347

PAT-347 is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood.

1689554-51-5
DC73763 CC-11050

Dovramilast (CC-11050) is a potent and orally active phosphodiesterase 4 (PDE4) inhibitor, CC-11050 is a promising candidate for host directed therapy of patients with pulmonary TB.

340019-69-4
DC73764 CRD733 Featured

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

917089-10-2
DC73765 Gemlapodect

Gemlapodect (NOE-105) is a potent, selective PDE10A inhibitor with a potential therapeutic effect for the treatment of COFD.

1380329-87-2
DC73766 MCI-030

MCI-030 (ADT 061) is a potent, selective PDE10 inhibitor, inhibits recombinant PDE10 using cGMP as a substrate with IC50 of 0.3 uM.

2700025-84-7
DC73767 ME3183

ME3183 is a potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 2.33, 1.28 and 1.63 nM for PDE4B1, PDE4A1A and PDE4D2 respectively.

2231329-25-0
DC73768 PF-2545920 hydrochloride

A potent and selective PDE10A inhibitor with IC50 of 0.37 nM.

DC73769 TOP-N53

TOP-N53 is a dual-acting nitric oxide (NO) donor and selective PDE5 inhibitor, potently inhibits PDE5 with IC50 of 1.6 nM.

2098499-23-9
DC73770 TPN171

TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.

1229018-87-4
DC73771 Yonkenafil

Yonkenafil is a potent, selective PDE5 inhibitor with IC50 of 2.0 nM.

804518-63-6
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