PLN-1474

PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Integrin

IC50: ＜50 nM (ανβ1), ＜50 nM (ανβ6)[1]

PLN-1474 inhibits ανβ1 and ανβ6 with IC50s of ＜50 nM by solid phase assay[1].

PLN-1474 (10 μM) decreases the expression level of profibrotic genes, including COL1A1 and TIMP1 in liver[1]. PLN-1474 significantly reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in a mouse model of liver fibrosis[1]. PLN-1474 (6-12 weeks) prophylactically or therapeutically blocks SMAD3 phosphorylation and significantly decreases OHP levels, collagen gene expression, and collagen deposition examined histologically in the CDAHFD NASH mouse model[1].

[1]. Anderson Kraig, et al. Combination treatment of liver diseases using integrin inhibitors. WO2021127483. 2021.