PDE

Inhibitory Selectivity

Isoform-specific Inhibitors

PDE Products

New PDE Products
Catalog No. Information Product Use Citations Product Validations
S0501

Enpp-1-IN-1

Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).

S6844

Zatolmilast (BPN14770)

Zatolmilast (BPN14770) is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.

S8895

Ziritaxestat (GLPG1690)

Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.

S7224

Deltarasin

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

E1205New

BAY 2666605

BAY 2666605 is an orally active phosphodiesterase 3A (PDE3A) and phosphodiesterase 3B (PDE3B) inhibitor with IC50s of 87 nM and 50 nM, respectively.

E0337New

MBCQ

MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE5) inhibitor with an IC50 of 19 nM.

E0423New

(R)-Avanafil

R-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM. 

E0617New

Lodenafil

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

E0346New

Ro 20-1724

Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues.

S0039

BI-409306

BI 409306 (SUB 166499) is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents.

S5894

Mirodenafil Dihydrochloride

Mirodenafil Dihydrochloride(SK-3530 dihydrochloride) is an oral phosphodiesterase type 5 (PDE-5) inhibitor used to treat erectile dysfunction (ED).

S5806

Cilostamide

Cilostamide (OPC 3689) is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively.

S6186

3-Methylxanthine

3-Methylxanthine (3-MX), a 3-alkylxanthine, is an inhibitor of cyclic guanosine monophosphate (GMP) phosphodiesterase (PDE) with IC50 of 920 μM on guinea-pig isolated trachealis muscle.

S5957

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.

S6576

BW-A78U

BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.

S2291

Diosgenin

Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills; A weak PDE inhibitor.

S2312

Icariin

Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.

S0127

CP-671305

CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.

S8218

PF-8380

PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.

S0190

Lotamilast (RVT-501)

Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

S5837

BRL-50481

BRL-50481 is a novel and selective inhibitor of phosphodiesterase (PDE) 7 with a Ki value, derived from secondary (Dixon) plots, of 180±10 nM, being at least 200-fold selective for hrPDE7A1 over all other PDEs.

S9229

Linderane

Linderane, isolated from Lindera strychnifolia vill., is an indirect PDE3 activator and possesses multiple biological effects, including superoxide anion radical-scavenging and antioxidative activity and protective activity against gastritis, gastric ulcers and backache.

E0483New

Calmidazolium chloride

Calmidazolium chloride (R 24571) is a calmodulin (CaM) antagonist, antagonizing CaM-stimulated fraction of rat brain phosphodiesterase and CaM-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively, also shows a CaM-binding Kd value of 3 nM.

Catalog No. Information Product Use Citations Product Validations
S0501

Enpp-1-IN-1

Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).

S6844

Zatolmilast (BPN14770)

Zatolmilast (BPN14770) is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.

S8895

Ziritaxestat (GLPG1690)

Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.

S7224

Deltarasin

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

E1205New

BAY 2666605

BAY 2666605 is an orally active phosphodiesterase 3A (PDE3A) and phosphodiesterase 3B (PDE3B) inhibitor with IC50s of 87 nM and 50 nM, respectively.

E0337New

MBCQ

MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE5) inhibitor with an IC50 of 19 nM.

E0423New

(R)-Avanafil

R-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM. 

E0617New

Lodenafil

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

E0346New

Ro 20-1724

Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues.

S0039

BI-409306

BI 409306 (SUB 166499) is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents.

S5894

Mirodenafil Dihydrochloride

Mirodenafil Dihydrochloride(SK-3530 dihydrochloride) is an oral phosphodiesterase type 5 (PDE-5) inhibitor used to treat erectile dysfunction (ED).

S5806

Cilostamide

Cilostamide (OPC 3689) is an inhibitor of type III phosphodiesterases with IC50 values of 27 nM and 50 nM for PDE3A and PDE3B, respectively.

S6186

3-Methylxanthine

3-Methylxanthine (3-MX), a 3-alkylxanthine, is an inhibitor of cyclic guanosine monophosphate (GMP) phosphodiesterase (PDE) with IC50 of 920 μM on guinea-pig isolated trachealis muscle.

S5957

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.

S6576

BW-A78U

BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.

S2291

Diosgenin

Diosgenin is a steroid sapogenin and the precursor for the semisynthesis of progesterone which in turn was used in early combined oral contraceptive pills; A weak PDE inhibitor.

S2312

Icariin

Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.

S0127

CP-671305

CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.

S8218

PF-8380

PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.

S0190

Lotamilast (RVT-501)

Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

S5837

BRL-50481

BRL-50481 is a novel and selective inhibitor of phosphodiesterase (PDE) 7 with a Ki value, derived from secondary (Dixon) plots, of 180±10 nM, being at least 200-fold selective for hrPDE7A1 over all other PDEs.

Catalog No. Information Product Use Citations Product Validations
S9229

Linderane

Linderane, isolated from Lindera strychnifolia vill., is an indirect PDE3 activator and possesses multiple biological effects, including superoxide anion radical-scavenging and antioxidative activity and protective activity against gastritis, gastric ulcers and backache.

Catalog No. Information Product Use Citations Product Validations
E0483New

Calmidazolium chloride

Calmidazolium chloride (R 24571) is a calmodulin (CaM) antagonist, antagonizing CaM-stimulated fraction of rat brain phosphodiesterase and CaM-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively, also shows a CaM-binding Kd value of 3 nM.