A 922500

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Chemical Structure| 959122-11-3 同义名 : DGAT-1 Inhibitor 4a; (1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)-cyclopentanecarboxylic acid; DGAT-1 inhibitor
CAS号 : 959122-11-3
货号 : A174946
分子式 : C26H24N2O4
纯度 : 98%
分子量 : 428.48
MDL号 : MFCD12828780
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

PO 5% DMSO + 30% PEG400 + 10% tween 80 + water 5 mg/mL clear

生物活性
靶点

  • Transferase

    mouse DGAT-1, IC50:24 nM

    human DGAT-1, IC50:7 nM
描述 A-922500 exhibits high selectivity against other acyltransferases, such as DGAT-2, with an IC50 value of 53 μM, and is also selective over its phylogenetic relatives, acyl coenzyme A cholesterol acyltransferase-1 and -2, with an IC50 value of 296 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.67mL

2.33mL

1.17mL

23.34mL

4.67mL

2.33mL
参考文献

[1]King AJ, Segreti JA, et al. In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61.

[2]Zhao G, Souers AJ, et al. Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J Med Chem. 2008 Feb 14;51(3):380-3.