tcsc7620 MGAT2-IN-1

MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC₅₀ of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

IC50 & Target: IC50: 7.8 nM (Human MGAT2), 2.4 nM (Mouse MGAT2)^[1]

In Vivo: MGAT2-IN-1 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG AUC in mice. MGAT2-IN-1 does not decrease MG absorption but inhibits MGAT2-dependent TG/DG resynthesis. In the lipid utilization analysis, MGAT2-IN-1 significantly increases free fatty acid (FFA) and acylcarnitine levels. MGAT2-IN-1 (30 mg/kg) also significantly reduces food intake dose dependently, suppresses BW gains. MGAT2-IN-1 shows anti-diabetic effects in mice^[1].