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PDE Phosphodiesterase

Inhibitors

Cat.No.  Name Information
M2030 Apremilast Apremilast is a novel, orally available small molecule inhibitor of PDE4 with IC50 of 74 nM.
M21352 Dovramilast Dovramilast (CC-11050) is a phosphodiesterase 4 (PDE4) inhibitor with oral activity that reduces the inflammatory response and improves Isoniazid (HY-B0329)-mediated clearance of bacteria from the lung.Dovramilast is used as an adjuvant in tuberculosis studies.
M21314 LEO 39652 LEO 39652 is a dual-soft PDE4 inhibitor with IC50 values of 1.2 nM for PDE4A, 1.2 nM for PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used in topical studies of atopic dermatitis.
M21275 ONO-8430506 ONO-8430506 is a potent autotaxin phosphodiesterase inhibitor with significant oral exposure and low clearance in higher species.
M21175 BIO-32546 Compound BIO-32546 is a potent (IC50=1 nM), selective, orally administered, non-zinc-binding reversible inhibitor of autophagy (ATX).
M20847 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.
M20723 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.
M20701 BPN14770 BPN14770 is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
M20590 BW-A78U BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity.
M20402 Mardepodect (PF-2545920) PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.
M20179 WAY-388796 WAY-388796 is a PDE5 inhibitor
M18283 Eurycomanone Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
M14507 Vardenafil Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM.
M14506 PF-04957325 PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.
M14505 PF-04447943 PF-04447943 is a potent inhibitor of human recombinant PDE9A (IC50=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC50>1000 nM).
M14504 ML-030 ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
M14503 GSK256066 Trifluoroacetate GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.
M14502 Deltasonamide 2 (TFA) Deltasonamide 2 TFA is competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
M14501 Deltasonamide 2 hydrochloride Deltasonamide 2 hydrochloride is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
M14500 Osoresnontrine Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.
M14499 (R)-(-)-Rolipram (R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.



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