TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerolacyltransferase(MGAT2) withIC₅₀of 7.8 and 2.4 nM for human and mouseMGAT2, respectively.

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

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^[1].

654.01

Solid

C₂₇H₂₁ClF₅N₇O₃S

1800025-30-2

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 125 mg/mL(191.13 mM)

*"≥" means soluble, but saturation unknown.

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