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Product details

名称

DGAT1-IN-3

分子类型

小分子

英文名称

DGAT1-IN-3

货号

D647241-5mg

包装规格

5mg

浓度

≥99%

储存温度

避光,-80℃储存

运输条件

超低温冰袋运输

产品介绍

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). Form:Solid IC50& Target:IC50: 38 nM (human DGAT-1),120 nM (rat DGAT-1)

生化机理

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。

CAS号

939375-07-2

分子式

C20H19F3N4O3

分子量

420.39 g/mol

PubChem编号

16757107

Isomeric SMILES

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

IIUPAC Name

N-[6-[2-methoxyethyl(methyl)amino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide

INCHI

1S/C20H19F3N4O3/c1-27(10-11-29-2)15-9-8-14(12-24-15)25-18(28)16-17(20(21,22)23)30-19(26-16)13-6-4-3-5-7-13/h3-9,12H,10-11H2,1-2H3,(H,25,28)

InChi Key

QEZWDFXCTTZZRI-UHFFFAOYSA-N

Smiles

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

PubChem CID

16757107

溶解性

DMSO : 100 mg/mL (237.87 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

420.141 Da

单同位素质量Monoisotopic Mass

420.141 Da

拓扑极表面积Topological Polar Surface Area

80.500 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

560.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.300

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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