PDE

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PDEシグナル伝達経路

PDE製品

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S7858 Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP,Dibutyryl cAMP sodium salt) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
Regen Ther, 2024, 25:229-237
Biology (Basel), 2024, 13(1)58
Nat Commun, 2023, 14(1):3212
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.
Sci Adv, 2024, 10(7):eadk1835
Cell Death Dis, 2023, 14(2):142
Phytomedicine, 2023, 120:155020
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.
J Pharm Pharmacol, 2023, rgad045
Phytomedicine, 2022, 102:154171
Int J Mol Med, 2022, 49(2)19
S4684 Sildenafil Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Brain, 2023, 146(6):2453-2463
Cardiovasc Res, 2021, 117(5):1391-1401
J Cell Physiol, 2020, 10.1002/jcp.29580
S2131 Roflumilast Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
Cancer Lett, 2022, 541:215749
Front Pharmacol, 2022, 13:865715
EMBO Rep, 2021, e51329
S1512 Tadalafil Tadalafil 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
S1430 Rolipram The PDE4 selective inhibitor, Rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.
Elife, 2022, 11e73511
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4
Antioxidants (Basel), 2021, 10(3)460
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.
J Hematol Oncol, 2023, 16(1):30
ACS Cent Sci, 2023, 9(4):719-732
Phytomedicine, 2023, 118:154942
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
S8034 Apremilast Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.
Signal Transduct Target Ther, 2023, 8(1):40
Acta Pharm Sin B, 2022, 12(1):228-245
Int J Mol Sci, 2021, 22(23)12878
S1294 Cilostazol (OPC-13013) Cilostazol (Pletal,OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
EBioMedicine, 2023, 95:104741
Platelets, 2023, 34(1):2173505
Cell Chem Biol, 2022, S2451-9456(22)00006-X
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
Am J Respir Cell Mol Biol, 2015, 52(5):634-40
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 Ovarian Res, 2022, 15(1):120
J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6
Am J Hum Genet, 2017, 100(1):5-20
S2312 Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.
Chinese Journal of Tissue Engineering Research, 2024, (28): 4461-4468.
Transl Oncol, 2023, 35:101712
J Orthop Surg Res, 2023, 18(1):500
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Eur J Cell Biol, 2023, 102(2):151314
Cell Death Differ, 2019, 26(11):2400-2415
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
S1895 Dipyridamole Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
Haematologica, 2023, 108(9):2343-2357
BIOCELL, 2023, 47(12): 2709-2719
Stem Cells, 2020, 38(8):1020-1033
S4683 Sildenafil Mesylate Sildenafil Mesylate(UK-92480 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
S8218 PF-8380 PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay.
J Clin Invest, 2023, 133(17)e163128
J Clin Invest, 2023, 133(17)e163128
Proc Natl Acad Sci U S A, 2023, 120(28):e2220276120
S1550 Pimobendan Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Front Microbiol, 2020, 10:2936
Sci Rep, 2020, 10(1):19723
Cell Syst, 2019, 8(2):97-108
S2484 Milrinone Milrinone (Win 47203,Primacor) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.
J Assist Reprod Genet, 2022, 10.1007/s10815-021-02330-x
Biochem Biophys Res Commun, 2018, 503(3):1409-1414
Mol Pharm, 2017, 10.1021/acs.molpharmaceut.7b00360
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.
Pharmaceuticals (Basel), 2022, 16(1)29
J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
S3172 Anagrelide HCl Anagrelide (BL-4162A,BMY 26538-01) is a drug used for the treatment of essential thrombocytosis.
Cell Chem Biol, 2022, S2451-9456(22)00006-X
Nat Cancer, 2020, 1(2):235-248
S0501 Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).
NPJ Breast Cancer, 2022, 8(1):44
Arthritis Res Ther, 2022, 24(1):44
S4837 Ibudilast Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
Front Psychiatry, 2023, 14:1259041
Neuron, 2020, 108(5):876-886.e4
CU Scholar, 2019, N/A
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.
Antiviral Res, 2023, 216:105674
Biogerontology, 2016, 17(5-6):907-920
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
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)
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
S1504 Dyphylline Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.
Biogerontology, 2016, 17(5-6):907-920
S4164 Doxofylline Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
J Immunother Cancer, 2022, 10(7)e004159
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
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
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.
Cells, 2021, 10(12)3502
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
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
S1929 Irsogladine Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S4090 Fenspiride HCl Fenspiride(Decaspiride) 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.
S5014 Crisaborole (AN2728) Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory 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.
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.
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.
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.
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.
S6576 BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
E0337 MBCQ MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE5) inhibitor with an IC50 of 19 nM.
E0617 Lodenafil Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
S0127 CP-671305 CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.
E0423 (R)-Avanafil R-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM. 
E1382New BI 1015550 BI 1015550 is an orally active inhibitor of PDE4B with IC50 of 7.2 nM. It has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).
S0424New HA130 HA130 is a selective autotaxin (ATX) inhibitor with IC50 of 28 nM.
S0190 Lotamilast (RVT-501) Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
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.
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.
E0483 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.
E0346 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.
E1205 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.
E2983New PF-04957325 PF-04957325 is a highly potent and selective inhibitor of PDE8, with IC50 values of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively. PF-04957325 greatly potentiates steroidogenesis in wild type adrenal cells.
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.
S3926 Forsythin Forsythin (FOR, Phillyrin) is an active ingredient extracted from the fruit of the medicinal plant Forsythia suspensa (Thunb.) Vahl and has been shown to have antioxidant, antibacterial and antiinflammatory properties.
S7858 Dibutyryl-cAMP (Bucladesine) Dibutyryl-cAMP (Bucladesine, dbcAMP,Dibutyryl cAMP sodium salt) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
Regen Ther, 2024, 25:229-237
Biology (Basel), 2024, 13(1)58
Nat Commun, 2023, 14(1):3212
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.
Sci Adv, 2024, 10(7):eadk1835
Cell Death Dis, 2023, 14(2):142
Phytomedicine, 2023, 120:155020
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.
J Pharm Pharmacol, 2023, rgad045
Phytomedicine, 2022, 102:154171
Int J Mol Med, 2022, 49(2)19
S4684 Sildenafil Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Brain, 2023, 146(6):2453-2463
Cardiovasc Res, 2021, 117(5):1391-1401
J Cell Physiol, 2020, 10.1002/jcp.29580
S2131 Roflumilast Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
Cancer Lett, 2022, 541:215749
Front Pharmacol, 2022, 13:865715
EMBO Rep, 2021, e51329
S1512 Tadalafil Tadalafil 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
S1430 Rolipram The PDE4 selective inhibitor, Rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.
Elife, 2022, 11e73511
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4
Antioxidants (Basel), 2021, 10(3)460
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.
J Hematol Oncol, 2023, 16(1):30
ACS Cent Sci, 2023, 9(4):719-732
Phytomedicine, 2023, 118:154942
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
S8034 Apremilast Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.
Signal Transduct Target Ther, 2023, 8(1):40
Acta Pharm Sin B, 2022, 12(1):228-245
Int J Mol Sci, 2021, 22(23)12878
S1294 Cilostazol (OPC-13013) Cilostazol (Pletal,OPC-13013) is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
EBioMedicine, 2023, 95:104741
Platelets, 2023, 34(1):2173505
Cell Chem Biol, 2022, S2451-9456(22)00006-X
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
Am J Respir Cell Mol Biol, 2015, 52(5):634-40
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 Ovarian Res, 2022, 15(1):120
J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6
Am J Hum Genet, 2017, 100(1):5-20
S2312 Icariin Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.
Chinese Journal of Tissue Engineering Research, 2024, (28): 4461-4468.
Transl Oncol, 2023, 35:101712
J Orthop Surg Res, 2023, 18(1):500
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Eur J Cell Biol, 2023, 102(2):151314
Cell Death Differ, 2019, 26(11):2400-2415
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
S1895 Dipyridamole Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
Haematologica, 2023, 108(9):2343-2357
BIOCELL, 2023, 47(12): 2709-2719
Stem Cells, 2020, 38(8):1020-1033
S4683 Sildenafil Mesylate Sildenafil Mesylate(UK-92480 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
S8218 PF-8380 PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay.
J Clin Invest, 2023, 133(17)e163128
J Clin Invest, 2023, 133(17)e163128
Proc Natl Acad Sci U S A, 2023, 120(28):e2220276120
S1550 Pimobendan Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Front Microbiol, 2020, 10:2936
Sci Rep, 2020, 10(1):19723
Cell Syst, 2019, 8(2):97-108
S2484 Milrinone Milrinone (Win 47203,Primacor) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.
J Assist Reprod Genet, 2022, 10.1007/s10815-021-02330-x
Biochem Biophys Res Commun, 2018, 503(3):1409-1414
Mol Pharm, 2017, 10.1021/acs.molpharmaceut.7b00360
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.
Pharmaceuticals (Basel), 2022, 16(1)29
J Aerosol Med Pulm Drug Deliv, 2019, 32(6):396-404
S3172 Anagrelide HCl Anagrelide (BL-4162A,BMY 26538-01) is a drug used for the treatment of essential thrombocytosis.
Cell Chem Biol, 2022, S2451-9456(22)00006-X
Nat Cancer, 2020, 1(2):235-248
S0501 Enpp-1-IN-1 Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).
NPJ Breast Cancer, 2022, 8(1):44
Arthritis Res Ther, 2022, 24(1):44
S4837 Ibudilast Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
Front Psychiatry, 2023, 14:1259041
Neuron, 2020, 108(5):876-886.e4
CU Scholar, 2019, N/A
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.
Antiviral Res, 2023, 216:105674
Biogerontology, 2016, 17(5-6):907-920
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
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)
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
S1504 Dyphylline Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.
Biogerontology, 2016, 17(5-6):907-920
S4164 Doxofylline Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
J Immunother Cancer, 2022, 10(7)e004159
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
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
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.
Cells, 2021, 10(12)3502
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
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
S1929 Irsogladine Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S4090 Fenspiride HCl Fenspiride(Decaspiride) 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.
S5014 Crisaborole (AN2728) Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory 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.
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.
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.
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.
S6576 BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
E0337 MBCQ MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE5) inhibitor with an IC50 of 19 nM.
E0617 Lodenafil Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
S0127 CP-671305 CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.
E0423 (R)-Avanafil R-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM. 
E1382New BI 1015550 BI 1015550 is an orally active inhibitor of PDE4B with IC50 of 7.2 nM. It has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).
S0424New HA130 HA130 is a selective autotaxin (ATX) inhibitor with IC50 of 28 nM.
S0190 Lotamilast (RVT-501) Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
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.
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.
E0346 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.
E1205 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.
E2983New PF-04957325 PF-04957325 is a highly potent and selective inhibitor of PDE8, with IC50 values of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively. PF-04957325 greatly potentiates steroidogenesis in wild type adrenal cells.
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.
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.
E0483 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.
E1382New BI 1015550 BI 1015550 is an orally active inhibitor of PDE4B with IC50 of 7.2 nM. It has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).
S0424New HA130 HA130 is a selective autotaxin (ATX) inhibitor with IC50 of 28 nM.
E2983New PF-04957325 PF-04957325 is a highly potent and selective inhibitor of PDE8, with IC50 values of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively. PF-04957325 greatly potentiates steroidogenesis in wild type adrenal cells.

PDE阻害剤の選択性比較

Tags: PDE inhibitor|PDE agonist|PDE activator|PDE inducer|PDE antagonist|PDE signaling pathway|PDE assay kit