DGAT1-IN-3

小分子

DGAT1-IN-3

D654941-1ml

1ml

10mM in DMSO

避光,-80℃储存

超低温冰袋运输

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 In Vitro DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC 20 of 0.2 μM. DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC 50 of 0.66 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile. 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. DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)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 ratsDosage: 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). IC50& Target:IC50: 38 nM (human DGAT-1),120 nM (rat DGAT-1)

DGAT1-IN-3 是一种强效、选择性和口服生物活性的 DGAT-1 抑制剂，对人 DGAT-1 的 IC 50 s 为 38 nM，对大鼠 DGAT-1 的 IC 50 s 为 120 nM。DGAT1-IN-3 可用于肥胖症、血脂异常和代谢综合征的研究。

939375-07-2(DMSO)

C20H19F3N4O3

420.39 g/mol

CN(CCOC)C1=NC=C(C=C1)NC(=O)C2=C(OC(=N2)C3=CC=CC=C3)C(F)(F)F