PDE

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

PDE Products

Catalog No. Information Product Use Citations Product Validations
S2131

Roflumilast

Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

S1431

Sildenafil Citrate

Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.

S1455

Cilomilast

Cilomilast (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.

S1512

Tadalafil

Tadalafil (IC351) is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11

S2515

Vardenafil HCl Trihydrate

Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

S6186New

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.

S6844New

BPN14770

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.

S0501New

Enpp-1-IN-1

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

S0127New

CP-671305

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

S0039New

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.

S4345New

Pentoxifylline

Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.

S8895New

Ziritaxestat (GLPG1690)

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

S1550

Pimobendan

Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

S2620

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 selectivity against PDE4B versus PDE7.Phase 2.

S2687

Mardepodect (PF-2545920)

Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

S1430

Rolipram

The PDE4 selective inhibitor, Rolipram (ZK-62711, SB 95952), inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.

S8034

Apremilast (CC-10004)

Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

S1294

Cilostazol

Cilostazol (OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.

S2484

Milrinone

Milrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.

S4019

Avanafil

Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

S2127

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 system, less potent than its R enantiomer.

S1673

Aminophylline

Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.

S3172

Anagrelide HCl

Anagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis.

S1504

Dyphylline

Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.

S1895

Dipyridamole

Dipyridamole (Persantine, NSC-515776) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.

S4164

Doxofylline

Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.

S4090

Fenspiride HCl

Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.

S4837

Ibudilast

Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.

S5014

Crisaborole (AN2728)

Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.

S7224

Deltarasin

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

S5806

Cilostamide

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

S5539

Olprinone

Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively.

S8459

TAK-063

TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.

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.

S4683

Sildenafil Mesylate

Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.

S4684

Sildenafil

Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

S2320

Luteolin

Luteolin is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. Phase 2.

S8218

PF-8380

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

S5836

IBMX

Isobutylmethylxanthine (IBMX) is a nonspecific inhibitor of phosphodiesterase (PDE) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. It may enhance the intracellular cAMP levels and also acts as an adenosine (A1) receptor antagonist.

S9436

Pinoresinol dimethyl ether

Pinoresinol dimethyl ether, which could be isolated from the wood of the basal tree Humbertieae, show a variety of activities as the inhibitor of cyclic AMP phosphodiesterase.

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.

S6433

Udenafil

Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.

S2368

Theobromine

Theobromine (3,7-Dimethylxanthine) is a xanthine alkaloid widely consumed as stimulants and snacks in coffee and cocoa based foods and most often as part of ingredients in drugs.

S7858

Dibutyryl-cAMP (Bucladesine)

Dibutyryl-cAMP (Bucladesine) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.

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
S2131

Roflumilast

Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

S1431

Sildenafil Citrate

Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.

S1455

Cilomilast

Cilomilast (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.

S1512

Tadalafil

Tadalafil (IC351) is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11

S2515

Vardenafil HCl Trihydrate

Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

S6186New

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.

S6844New

BPN14770

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.

S0501New

Enpp-1-IN-1

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

S0127New

CP-671305

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

S0039New

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.

S4345New

Pentoxifylline

Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.

S8895New

Ziritaxestat (GLPG1690)

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

S1550

Pimobendan

Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

S2620

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 selectivity against PDE4B versus PDE7.Phase 2.

S2687

Mardepodect (PF-2545920)

Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

S1430

Rolipram

The PDE4 selective inhibitor, Rolipram (ZK-62711, SB 95952), inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.

S8034

Apremilast (CC-10004)

Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

S1294

Cilostazol

Cilostazol (OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.

S2484

Milrinone

Milrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.

S4019

Avanafil

Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

S2127

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 system, less potent than its R enantiomer.

S1673

Aminophylline

Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.

S3172

Anagrelide HCl

Anagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis.

S1504

Dyphylline

Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.

S1895

Dipyridamole

Dipyridamole (Persantine, NSC-515776) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.

S4164

Doxofylline

Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.

S4090

Fenspiride HCl

Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.

S4837

Ibudilast

Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.

S5014

Crisaborole (AN2728)

Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.

S7224

Deltarasin

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

S5806

Cilostamide

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

S5539

Olprinone

Olprinone is a phosphodiesterase III (PDE3) inhibitor with IC50 values of 0.35 mM, 150 mM and 100 mM for human cardiac PDE III, PDE I and PDE II, respectively.

S8459

TAK-063

TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.

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.

S4683

Sildenafil Mesylate

Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.

S4684

Sildenafil

Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

S2320

Luteolin

Luteolin is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. Phase 2.

S8218

PF-8380

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

S5836

IBMX

Isobutylmethylxanthine (IBMX) is a nonspecific inhibitor of phosphodiesterase (PDE) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. It may enhance the intracellular cAMP levels and also acts as an adenosine (A1) receptor antagonist.

S9436

Pinoresinol dimethyl ether

Pinoresinol dimethyl ether, which could be isolated from the wood of the basal tree Humbertieae, show a variety of activities as the inhibitor of cyclic AMP phosphodiesterase.

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.

S6433

Udenafil

Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.

S2368

Theobromine

Theobromine (3,7-Dimethylxanthine) is a xanthine alkaloid widely consumed as stimulants and snacks in coffee and cocoa based foods and most often as part of ingredients in drugs.

S7858

Dibutyryl-cAMP (Bucladesine)

Dibutyryl-cAMP (Bucladesine) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.

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.