DGAT1-IN-3 是一种有效的，选择性的，具有口服活性的DGAT-1抑制剂，抑制人类和大鼠DGAT-1的IC50值分别为 38 nM 和 120 nM。DGAT1-IN-3 可用于研究肥胖，血脂异常和代谢综合征。

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC 50 s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome [1] [2].

DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC 20 of 0.2 μM [1]. DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC 50 of 0.66 μM [1].

DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile [2]. DGAT1-IN-3 (50 mg/kg; p.o) exhibits good oral bioavailability (77%) and the maximum exposure level in plasma (C max ) is 24 μM [2]. DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg) [2]. Animal Model: Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet) [2] Dosage: 0, 5, 25, 50 mg/kg; once daily for three weeks Administration: P.o. administration Result: Reduced cumulative body weight gain in a dose-dependent manner and was well tolerated in rats. Animal Model: Male Wistar rats [2] Dosage: 50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis) Administration: P.o. and i.v. administration Result: C max (24 μM); T 1/2 (1.95 h).

939375-07-2

C20H19F3N4O3

420.39

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years