PDE1-IN-4 

PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC₅₀ values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research^[1].

PDE1-IN-4 (compound 2g) shows weak inhibition against the hERG channel with an IC₅₀ above 40 μM, indicating that it will not cause cardiotoxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

535.63

C₃₃H₃₃N₃O₄

3031349-98-8

CC1=C(C(C2=CC3=C(C=C2)N(N=C3)C)C(C(O[C@@H](C4=CC=CC=C4)C)=O)=C(N1)C)C(O[C@@H](C5=CC=CC=C5)C)=O

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• [1]. Huang MX, et al. Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects. J Med Chem. 2022 Jun 23;65(12):8444-8455.  [Content Brief]