Pradigastat (sodium)

Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC₅₀ at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC₅₀ of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro^[1][2][3][4]. IC50 & Target:Diacylglycerol acyltransferase 1 (DGAT1)^[1]
IC₅₀: 5 µM (BCRP); IC₅₀: 1.66 µM (OATP1B1); IC₅₀: 3.34 µM (OATP1B3); IC₅₀: 0.973 µM (OAT3)^[2] In Vitro:Pradigastat (0-50 μM; 1 h) inhibits BCRP-mediated efflux activity in a dose-dependent manner in overexpressing human ovarian cancer cell lines with an IC₅₀ of 5 µM^[2].
Pradigastat (0-50 μM; 5 minutes) inhibits OATP1B1, OATP1B3, and OAT3 activities in a concentration-dependent manner with IC₅₀ of 1.66µM, 3.34µM and 0.973µM, respectively^[2].
Pradigastat (2-20 μM; 8 h) inhibits the replication and production of hepatitis C virus in vitro^[3].