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Catalog No. Product Name Information Product Use Citations Product Validations
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.
S0127 CP-671305 CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.
S0501 Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).
S1294 Cilostazol (OPC-13013) Cilostazol (OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
Front Pharmacol, 2021, 12:749930
Front Cell Infect Microbiol, 2021, 11:783085
Int J Biol Sci, 2020, 27;16(11):2001-2013
S1430 Rolipram (ZK-62711) 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.
Antioxidants (Basel), 2021, 10(3)460
Sci Rep, 2021, 11(1):19737
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4
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.
Int J Mol Med, 2022, 49(2)19
J Clin Invest, 2021, 131(1)136779
Cardiovasc Res, 2021, 117(5):1391-1401
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.
Am J Physiol Renal Physiol, 2020, 318(3):F576-F588
J Pharm Biomed Anal, 2016, 117:47-60
Mol Cancer Res, 2015, 13(1):149-60
S1504 Dyphylline Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.
Biogerontology, 2016, 17(5-6):907-920
S1512 Tadalafil (IC351) 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
J Clin Invest, 2021, 131(1)136779
Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267
Mol Biochem Parasitol, 2021, 244:111392
S1550 Pimobendan Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Sci Rep, 2020, 10(1):19723
Front Microbiol, 2020, 10:2936
Cell Syst, 2019, 8(2):97-108
S1673 Aminophylline Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.
Gastroenterology, 2020, 159(3):1068-1084.e2
S1895 Dipyridamole (NSC 515776) Dipyridamole (NSC-515776, Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
Stem Cells, 2020, 38(8):1020-1033
Stem Cells, 2020, 28
Am J Hum Genet, 2017, 100(1):5-20
S1929 Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
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.
Viruses, 2019, 11(12)
S2131 Roflumilast (B9302-107) 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.
EMBO Rep, 2021, e51329
Free Radic Biol Med, 2021, 163:281-296
Mol Cell, 2020, 80(6):1104-1122.e9
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.
Neurochem Res, 2020, 10.1007/s11064-020-03093-0
S2312 Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.
Phytomedicine, 2021, 80:153387
Br J Nutr, 2021, 1-11
J Med Virol, 2019, 91(8):1440-1447
S2320 Luteolin Luteolin (Luteoline, Luteolol, Digitoflavone) 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.
Cancer Lett, 2021, 515:36-48
Molecules, 2021, 26(5)1210
Am J Cancer Res, 2021, 11(2):458-478
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.
S2484 Milrinone Milrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.
Biochem Biophys Res Commun, 2018, 503(3):1409-1414
Mol Pharm, 2017, 10.1021/acs.molpharmaceut.7b00360
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.
Gastroenterology, 2020, 159(3):1068-1084.e2
Bone, 2020, 10.1016/j.bone.2020.115305
Pulm Pharmacol Ther, 2020, 66:101985
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.
J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
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.
J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6
Front Mol Neurosci, 2017, 10:100
Oncotarget, 2017, 8(41):69264-69280
S3172 Anagrelide HCl Anagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis.
Nat Cancer, 2020, 1(2):235-248
S4019 Avanafil Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
Cell Rep, 2021, 37(1):109774
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.
S4164 Doxofylline Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
S4345 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.
Biogerontology, 2016, 17(5-6):907-920
S4683 Sildenafil Mesylate Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
Cardiovasc Res, 2021, 117(5):1391-1401
Sci Rep, 2020, 10(1):18084
Oncotarget, 2016, 7(11):12975-96
S4684 Sildenafil Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Cardiovasc Res, 2021, 117(5):1391-1401
J Cell Physiol, 2020, 10.1002/jcp.29580
Bone, 2020, 10.1016/j.bone.2020.115305
S4837 Ibudilast Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
Neuron, 2020, 108(5):876-886.e4
CU Scholar, 2019, N/A
S5014 Crisaborole (AN2728) Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
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.
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.
S5836 IBMX IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) 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.
PLoS One, 2019, 14(3):e0214554
Toxicology, 2018, 394:1-10
Cell Death Dis, 2016, 7:e2152
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.
Oncogene, 2017, 36(23):3252-3262
S5957New 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.
Cells, 2021, 10(12)3502
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.
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.
S6576 BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
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.
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
Cell Death Differ, 2019, 26(11):2400-2415
Nat Commun, 2018, 9(1):672
S7858 Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
Nat Commun, 2021, 12(1):4050
EMBO Mol Med, 2021, e12632
Cell Rep, 2021, 37(12):110137
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.
Int J Mol Sci, 2021, 22(23)12878
J Immunotoxicol, 2021, 18(1):154-162
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.04.007
S8218 PF-8380 PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.
Leuk Lymphoma, 2021, 1-12
S8459 TAK-063 TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.
Int J Mol Sci, 2021, 22(18)9665
S8895 Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.
Front Cell Dev Biol, 2021, 9:656153
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.
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.
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.
S0127 CP-671305 CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.
S0501 Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).
S1294 Cilostazol (OPC-13013) Cilostazol (OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
Front Pharmacol, 2021, 12:749930
Front Cell Infect Microbiol, 2021, 11:783085
Int J Biol Sci, 2020, 27;16(11):2001-2013
S1430 Rolipram (ZK-62711) 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.
Antioxidants (Basel), 2021, 10(3)460
Sci Rep, 2021, 11(1):19737
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4
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.
Int J Mol Med, 2022, 49(2)19
J Clin Invest, 2021, 131(1)136779
Cardiovasc Res, 2021, 117(5):1391-1401
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.
Am J Physiol Renal Physiol, 2020, 318(3):F576-F588
J Pharm Biomed Anal, 2016, 117:47-60
Mol Cancer Res, 2015, 13(1):149-60
S1504 Dyphylline Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.
Biogerontology, 2016, 17(5-6):907-920
S1512 Tadalafil (IC351) 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
J Clin Invest, 2021, 131(1)136779
Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267
Mol Biochem Parasitol, 2021, 244:111392
S1550 Pimobendan Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Sci Rep, 2020, 10(1):19723
Front Microbiol, 2020, 10:2936
Cell Syst, 2019, 8(2):97-108
S1673 Aminophylline Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.
Gastroenterology, 2020, 159(3):1068-1084.e2
S1895 Dipyridamole (NSC 515776) Dipyridamole (NSC-515776, Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
Stem Cells, 2020, 38(8):1020-1033
Stem Cells, 2020, 28
Am J Hum Genet, 2017, 100(1):5-20
S1929 Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
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.
Viruses, 2019, 11(12)
S2131 Roflumilast (B9302-107) 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.
EMBO Rep, 2021, e51329
Free Radic Biol Med, 2021, 163:281-296
Mol Cell, 2020, 80(6):1104-1122.e9
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.
Neurochem Res, 2020, 10.1007/s11064-020-03093-0
S2312 Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.
Phytomedicine, 2021, 80:153387
Br J Nutr, 2021, 1-11
J Med Virol, 2019, 91(8):1440-1447
S2320 Luteolin Luteolin (Luteoline, Luteolol, Digitoflavone) 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.
Cancer Lett, 2021, 515:36-48
Molecules, 2021, 26(5)1210
Am J Cancer Res, 2021, 11(2):458-478
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.
S2484 Milrinone Milrinone (Win 47203) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.
Biochem Biophys Res Commun, 2018, 503(3):1409-1414
Mol Pharm, 2017, 10.1021/acs.molpharmaceut.7b00360
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.
Gastroenterology, 2020, 159(3):1068-1084.e2
Bone, 2020, 10.1016/j.bone.2020.115305
Pulm Pharmacol Ther, 2020, 66:101985
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.
J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
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.
J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6
Front Mol Neurosci, 2017, 10:100
Oncotarget, 2017, 8(41):69264-69280
S3172 Anagrelide HCl Anagrelide (BL-4162A) is a drug used for the treatment of essential thrombocytosis.
Nat Cancer, 2020, 1(2):235-248
S4019 Avanafil Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.
Cell Rep, 2021, 37(1):109774
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.
S4164 Doxofylline Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
S4345 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.
Biogerontology, 2016, 17(5-6):907-920
S4683 Sildenafil Mesylate Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
Cardiovasc Res, 2021, 117(5):1391-1401
Sci Rep, 2020, 10(1):18084
Oncotarget, 2016, 7(11):12975-96
S4684 Sildenafil Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Cardiovasc Res, 2021, 117(5):1391-1401
J Cell Physiol, 2020, 10.1002/jcp.29580
Bone, 2020, 10.1016/j.bone.2020.115305
S4837 Ibudilast Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
Neuron, 2020, 108(5):876-886.e4
CU Scholar, 2019, N/A
S5014 Crisaborole (AN2728) Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
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.
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.
S5836 IBMX IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) 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.
PLoS One, 2019, 14(3):e0214554
Toxicology, 2018, 394:1-10
Cell Death Dis, 2016, 7:e2152
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.
Oncogene, 2017, 36(23):3252-3262
S5957New 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.
Cells, 2021, 10(12)3502
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.
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.
S6576 BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
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.
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
Cell Death Differ, 2019, 26(11):2400-2415
Nat Commun, 2018, 9(1):672
S7858 Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
Nat Commun, 2021, 12(1):4050
EMBO Mol Med, 2021, e12632
Cell Rep, 2021, 37(12):110137
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.
Int J Mol Sci, 2021, 22(23)12878
J Immunotoxicol, 2021, 18(1):154-162
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.04.007
S8218 PF-8380 PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.
Leuk Lymphoma, 2021, 1-12
S8459 TAK-063 TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.
Int J Mol Sci, 2021, 22(18)9665
S8895 Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM.
Front Cell Dev Biol, 2021, 9:656153
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.
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.
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.

S5957New 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.
Cells, 2021, 10(12)3502