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. |
-
Cell Rep Med, 2024, 5(3):101477
-
ACS Appl Mater Interfaces, 2024, 16(40):54292-54303
-
Commun Biol, 2024, 7(1):1393
|
|
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. |
-
Adv Sci (Weinh), 2024, 11(40):e2407712
-
J Immunother Cancer, 2024, 12(11)e009805
-
Brain, 2023, 146(6):2453-2463
|
|
S2131 |
Roflumilast
|
Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay. |
-
Respir Investig, 2024, 62(3):455-461
-
Cancer Lett, 2022, 541:215749
-
Front Pharmacol, 2022, 13:865715
|
|
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 Immunother Cancer, 2024, 12(11)e009805
-
J Clin Invest, 2021, 131(1)136779
-
Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267
|
|
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
-
J Hematol Oncol, 2023, 16(1):30
-
ACS Cent Sci, 2023, 9(4):719-732
|
|
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
|
Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
EBioMedicine, 2023, 95:104741
-
Platelets, 2023, 34(1):2173505
|
|
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. |
-
J Vet Res, 2024, 68(1):35-44
-
Chinese Journal of Tissue Engineering Research, 2024, (28): 4461-4468.
-
Transl Oncol, 2023, 35:101712
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Heliyon, 2024, 10(1):e23831
-
Haematologica, 2023, 108(9):2343-2357
|
|
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 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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Front Microbiol, 2020, 10:2936
-
Sci Rep, 2020, 10(1):19723
|
|
S2484 |
Milrinone
|
Milrinone (Win 47203,Primacor) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
J Assist Reprod Genet, 2022, 10.1007/s10815-021-02330-x
-
Pharmaceuticals (Basel), 2021, 14(7)697
|
|
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
-
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). |
-
Acta Pharmacol Sin, 2024,
-
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
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. |
-
Front Pharmacol, 2024, 15:1411652
-
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. |
|
|
E4695New |
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). |
|
|
E4979New |
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. |
|
|
E4924New |
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. |
|
|
E4803New |
Vardenafil
|
Vardenafil is an orally active and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 value of 0.7 nM, respectively. Vardenafil acts as a competitive inhibitor of cyclic guanosine monophosphate (cGMP) hydrolysis, thereby increasing cGMP levels. Vardenafil 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. |
|
|
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
|
|
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. |
|
|
E4843New |
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. |
|
|
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
|
|
E4793New |
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. |
|
|
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 |
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). |
|
|
S0424 |
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. |
- Cell Rep Med, 2024, 5(3):101477
- ACS Appl Mater Interfaces, 2024, 16(40):54292-54303
- Commun Biol, 2024, 7(1):1393
|
|
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. |
- Adv Sci (Weinh), 2024, 11(40):e2407712
- J Immunother Cancer, 2024, 12(11)e009805
- Brain, 2023, 146(6):2453-2463
|
|
S2131 |
Roflumilast
|
Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay. |
- Respir Investig, 2024, 62(3):455-461
- Cancer Lett, 2022, 541:215749
- Front Pharmacol, 2022, 13:865715
|
|
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 Immunother Cancer, 2024, 12(11)e009805
- J Clin Invest, 2021, 131(1)136779
- Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267
|
|
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
- J Hematol Oncol, 2023, 16(1):30
- ACS Cent Sci, 2023, 9(4):719-732
|
|
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
|
Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake. |
- J Immunother Cancer, 2024, 12(11)e009805
- EBioMedicine, 2023, 95:104741
- Platelets, 2023, 34(1):2173505
|
|
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. |
- J Vet Res, 2024, 68(1):35-44
- Chinese Journal of Tissue Engineering Research, 2024, (28): 4461-4468.
- Transl Oncol, 2023, 35:101712
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Heliyon, 2024, 10(1):e23831
- Haematologica, 2023, 108(9):2343-2357
|
|
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 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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Front Microbiol, 2020, 10:2936
- Sci Rep, 2020, 10(1):19723
|
|
S2484 |
Milrinone
|
Milrinone (Win 47203,Primacor) is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility. |
- J Immunother Cancer, 2024, 12(11)e009805
- J Assist Reprod Genet, 2022, 10.1007/s10815-021-02330-x
- Pharmaceuticals (Basel), 2021, 14(7)697
|
|
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
- 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). |
- Acta Pharmacol Sin, 2024,
- 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. |
- J Immunother Cancer, 2024, 12(11)e009805
- 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. |
- Front Pharmacol, 2024, 15:1411652
- 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. |
|
|
E4979New |
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. |
|
|
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. |
|
|
E4924New |
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. |
|
|
E4803New |
Vardenafil
|
Vardenafil is an orally active and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 value of 0.7 nM, respectively. Vardenafil acts as a competitive inhibitor of cyclic guanosine monophosphate (cGMP) hydrolysis, thereby increasing cGMP levels. Vardenafil 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. |
|
|
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
|
|
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. |
|
|
E4843New |
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. |
|
|
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
|
|
E4793New |
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. |
|
|
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 |
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). |
|
|
S0424 |
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. |
|
|