IC50: <50 nM (αΝβ1), <50 nM (αΝβ6)[1]
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].
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.