PDE Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2312	Icariin	Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.	Naunyn Schmiedebergs Arch Pharmacol, 2025, none J Vet Res, 2024, 68(1):35-44 Chinese Journal of Tissue Engineering Research, 2024, (28): 4461-4468.
S1455	Cilomilast	Cilomomilast (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.	Biochim Biophys Acta Mol Basis Dis, 2025, 1871(1):167526 Am J Physiol Renal Physiol, 2020, 318(3):F576-F588 J Pharm Biomed Anal, 2016, 117:47-60
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
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
S2484	Milrinone	Milrinone (Win 47203, Primacor) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.	BMC Genomics, 2025, 26(1):270 J Immunother Cancer, 2024, 12(11)e009805 J Assist Reprod Genet, 2022, 10.1007/s10815-021-02330-x
S7224	Deltarasin	Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with K_d of 38 nM for binding to purified PDEδ.	Eur J Cell Biol, 2023, 102(2):151314 Appl. Sci, 2023, 13(1), 166 Cell Death Differ, 2019, 26(11):2400-2415
S1550	Pimobendan	Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.	Autophagy, 2025, 1-17. J Immunother Cancer, 2024, 12(11)e009805 Front Microbiol, 2020, 10:2936
S0501	Enpp-1-IN-1	Enpp-1-IN-1 (UUN28589, MV 658) is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1).	Cell Rep, 2025, 44(6):115851 iScience, 2025, 28(3):111943 Acta Pharmacol Sin, 2024,
S4683	Sildenafil Mesylate	Sildenafil Mesylate(UK-92480 Mesylate) is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.	J Immunother Cancer, 2024, 12(11)e009805 Cardiovasc Res, 2021, 117(5):1391-1401 Sci Rep, 2020, 10(1):18084
S8218	PF-8380	PF-8380 is a potent autotaxin (ATX) inhibitor with IC50 of 2.8 nM in an in vitro enzyme assay.	Cell Mol Biol Lett, 2024, 29(1):159 Front Immunol, 2024, 15:1481699 J Clin Invest, 2023, 133(17)e163128
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
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.	Cell Rep Med, 2025, 6(9):102356 Front Pharmacol, 2024, 15:1411652 Oncogene, 2017, 36(23):3252-3262
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
S4019	Avanafil	Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.	J Immunother Cancer, 2024, 12(11)e009805 Cell Rep, 2021, 37(1):109774
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
S1504	Dyphylline	Dyphylline (Diprophylline) is a xanthine derivative with bronchodilator and vasodilator effects.	Cancer Cell, 2025, 43(4):776-796.e14 Biogerontology, 2016, 17(5-6):907-920
S4164	Doxofylline	Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.	Toxicol Lett, 2025, 406:31-37 J Immunother Cancer, 2022, 10(7)e004159
S8459	TAK-063	TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.	Alzheimers Res Ther, 2025, 17(1):231 Int J Mol Sci, 2021, 22(18)9665
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.	Biochem Biophys Rep, 2025, 42:102021 Neurochem Res, 2020, 10.1007/s11064-020-03093-0
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
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
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.	Br J Pharmacol, 2024, 10.1111/bph.17411
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
E4924	Anagrelide	Anagrelide(BL416201), an imidazoquinazoline derivative, is an inhibitor of phosphodiesterase type III (PDEIII) with IC50 of 36 nM, which acts as an antithrombotic and platelet-reducing agent.	Toxicol Lett, 2025, 406:31-37
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.	J Immunother Cancer, 2024, 12(11)e009805
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
S0424	HA130	HA130 is a selective autotaxin (ATX) inhibitor with IC50 of 28 nM.	Cell Rep, 2024, 43(11):114972
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.	J Nanobiotechnology, 2025, 23(1):173
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.
E4986	Mirodenafil	Mirodenafil (SK3530) is a second-generation, highly selective inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.34 nM, primarily used in the treatment of erectile dysfunction (ED).
S5014	Crisaborole (AN2728)	Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
E4695	OPB-171775	OPB-171775 functions as a molecular glue, promoting the formation of a complex between phosphodiesterase 3A (PDE3A) and Schlafen family member 12 (SLFN12). This interaction triggers multiple cellular stresses, ultimately leading to cell death. It also demonstrates significant anticancer activity in patient-derived xenograft (PDX) models of Gastrointestinal stromal tumor (GIST).
E4979	Olprinone Hydrochloride	Olprinone hydrochloride(Loprinone Hydrochloride, E-1020) is a potent inhibitor of phosphodiesterase (PDE) 3, with an IC50 value of 0.35 μM for PDE3, respectively. Olprinone Hydrochloride is used in the research of heart failure treatment due to its positive inotropic and vasodilatory effects. It also exhibits anti-inflammatory properties.
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.
E4803	Vardenafil	Vardenafil is an orally active and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 value of 0.7 nM, respectively. This compound acts as a competitive inhibitor of cyclic guanosine monophosphate (cGMP) hydrolysis, thereby increasing cGMP levels. It can be used for the research of erectile dysfunction, hepatitis, diabetes.
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.
S6576	BW-A78U	BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
E7654	Mardepodect	Mardepodect is a potent, orally active, and selective inhibitor of PDE10A with an IC50 of 0.37 nM and >1000-fold selectivity over other phosphodiesterases. It also suppresses microglial activation in LPS-induced neuroinflammation and MPTP-induced Parkinson's disease mouse models.
E4843	Vardenafil dihydrochloride	Vardenafil dihydrochloride is a potent, and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. It also exhibits inhibition of PDE1 and PDE6 with IC50 of 180 nM and 11 nM respectively. It can be used for the research of erectile dysfunction, hepatitis, diabetes.
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.
E1382	Nerandomilast (BI 1015550)	Nerandomilast (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).
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.
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.
E2983	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. This compound greatly potentiates steroidogenesis in wild type adrenal cells.
E1566^New	Ensifentrine	Ensifentrine (RPL-554) is a first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50 values of 0.4 nM and 1479 nM, respectively. Ensifentrine also inhibits lipopolysaccharide-induced tumor necrosis factor alpha release from human monocytes in a concentration-dependent manner. Ensifentrine demonstrates bronchoprotective and anti-inflammatory activities and can be used for chronic obstructive pulmonary disease (COPD) research.
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.
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.	Int Immunopharmacol, 2025, 144:113612 Front Nutr, 2025, 12:1552890 BMC Cancer, 2025, 25(1):411
E4793	Bucladesine calcium	Bucladesine calcium (Dibutyryl-cAMP Calcium Salt, DBcAMP calcium salt) is a cell-permeable analog of cyclic AMP. It serves as a potent activator of protein kinase A (PKA) and mimics the effects of endogenous cAMP. It also inhibits phosphodiesterase (PDE) activity, with the potential to treat congestive heart failure, wound healing, and inflammation.	Regen Ther, 2025, 29:499-505
E8284^New	PM534	PM534 is a potent microtubule-targeting agent (MTA) that binds the colchicine-binding domain (CBD) and inhibits tubulin assembly with IC50 values ranging from 0.8 to 3.2 nM. It also significantly inhibits tumor growth in mouse xenograft models of human non-small cell lung cancer.