pde4d2

PDE9-IN-(S)-C33 ((S)-C33) is a potent and selective inhibitor of PDE9 (IC50 = 11 nM). PDE9-IN-(S)-C33 can be used for central nervous system diseases and diabetes research.

PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5 (IC50 of 0.31 nM).

PDE4-IN-30 is a selective PDE4 inhibitor with an IC50 of 2.7 nM for PDE4D2, targeting PDE4 through halogen bonding and metal coordination. It demonstrates at least 67 times greater selectivity for PDE4 compared to other PDE subfamilies and is applicable in research for idiopathic pulmonary fibrosis.

LH17 is a derivative of Kaempferol and serves as a potent and selective inhibitor of PDE4, with PDE4D2 IC50 at 73 nM and PDE4B2 IC50 at 190 nM. It demonstrates over 136-fold selectivity against other PDE isoenzymes (PDE1B/2A/3A/5A/8A/9A/10A) with IC50s greater than 10000 nM, except for PDE7A1 which has an IC50 of 300 nM. LH17 exhibits unique interactions with the M pocket of PDE4. In vitro and in vivo models show that LH17 has significant antifibrotic effects. This compound is applicable in the study of idiopathic pulmonary fibrosis (IPF).

LEO-32731 is a bioactive chemical.

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

PDE4-IN-12 is a potent and safe ubiquitous PDE4 inhibitor with an IC50 of 3.5 nM (SI: 2.71) and also acts on PDE7 with an IC50 of 15 nM (SI: 4.27).

Moracin M, a phenolic compound found in the skin of Morus alba Linn., effectively inhibits phosphodiesterase-4 (PDE4), exhibiting IC50 values of 2.9 μM and 4.5 μM for PDE4D2 and PDE4B2, respectively, and showing significantly lesser activity on PDE5A1 and PDE9A2 with values over 40 μM and 100 μM, respectively. This compound demonstrates notable anti-inflammatory activity.

Norbraylin is a natural product from Toddalia asiatica.

ML-030 is a potent and selective inhibitor of PDE4(PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2 with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM, respectively)