产品
编 号：F609556
分子式：C20H19F3N4O3
分子量：420.39
分子式：C20H19F3N4O3
分子量：420.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 939375-07-2
产品详情
生物活性：
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s 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.
体内研究：
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 (Cmax) 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).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 rats
Dosage:50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:P.o. and i.v. administration
Result:Cmax (24 μM); T1/2 (1.95 h).
体外研究：
DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM.DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC50 of 0.66 μM.
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s 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.
体内研究：
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 (Cmax) 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).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 rats
Dosage:50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:P.o. and i.v. administration
Result:Cmax (24 μM); T1/2 (1.95 h).
体外研究：
DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM.DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC50 of 0.66 μM.
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