DGAT1-IN-3|939375-07-2|-陌孚医药/Medlife

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DGAT1-IN-3

目录号: PL14714 纯度: ≥99%

CAS No. :939375-07-2

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中文名称	DGAT1-IN-3
英文名称	DGAT1-IN-3
英文别名	DGAT1-IN-3;BDBM50341760;2-phenyl-5-trifluoromethyl-oxazole-4-carboxylic acid {6-[(2-methoxy-ethyl)-methyl-amino]-pyridin-3-yl}-amide;2-Phenyl-5-trifluoromethyloxazole-4-carboxylic Acid{6-[(2-Methoxyethyl)methylamino]pyridin-3-yl}amide;N-[6-[2-methoxyethyl(methyl)amino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide;N-[6-[(2-Methoxyethyl)methylamino]-3-pyridinyl]-2-phenyl-5-(trifluoromethyl)-4-oxazolecarboxamide (ACI)
Cas No.	939375-07-2
分子式	C₂₀H₁₉F₃N₄O₃
分子量	420.39
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	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。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	IC50: 38 nM (human DGAT-1); 120 nM (rat DGAT-1)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献	[1]. Yimin Q, et, al. Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem. 2011 Apr 14; [2]. Weiya Y, et, al. Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors. Bioorg Med Chem Lett. 2011 Dec 1; 21(23): 7205-9.

溶解度数据	In Vitro: DMSO : 100 mg/mL (237.87 mM; Need ultrasonic)配制储备液

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