TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC 50 of 7.8 and 2.4 nM for human and mouse MGAT2 , respectively.
In Vivo
TP-020 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG AUC in mice. TP-020 does not decrease MG absorption but inhibits MGAT2-dependent TG/DG resynthesis. In the lipid utilization analysis, TP-020 significantly increases free fatty acid (FFA) and acylcarnitine levels. TP-020 (30 mg/kg) also significantly reduces food intake dose dependently, suppresses BW gains. TP-020 shows anti-diabetic effects in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
