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CAS No.: 943962-47-8

BMS-303141 Catalog No. CSN18618

Synonyms: BMS-303141

BMS-303141 is a potent ATPcitrate lyase (ACL) inhibitor with IC50 of 0.13 μM (human recombinant ACL).

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述ATP-citratelyase (ACL) is an extramitochondrial enzyme that is expressed in lipogenic tissues such as liver and adipose. And it's responsible for the production of cytosolic acetyl-CoA, a precursor required for de novo biosyntheses of cholesterol and fatty acids. BMS-303141 is an ACL inhibitor displaying potent in vitro activity (IC₅₀ = 0.13 μM). And it showed inhibition of total lipid syntheses with an IC₅₀ of 8 μM in HepG2 cells. In mice, BMS-303141 showed an oral bioavailability of 55% and a half-life of 2.1 hr. Two high-fat diet mice groups were supplemented with BMS-303141 to an equivalent daily dose of 10 or100 mg/kg for 34 days. There was a modest lowering of both plasma cholesterol and triglycerides after 20 days of treatment. A reduction in fasting plasma glucose was observed from day 7 to completion of the study. At day 29, cholesterol was lowered by 19% with the 100 mg/kg dose and triglycerides were lowered by 26% in both the 10 and 100 mg/kg treatment groups. Fasting plasma glucose was lowered by 48% and 32% for 10 and100 mg/kg doses, respectively^[3].
动物研究
剂量
Mice: 10 mg/kg, 100 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 10 mg/kg, 100 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Ma Z, Chu CH, Cheng D. A novel direct homogeneous assay for ATP citrate lyase. J Lipid Res. 2009 Oct;50(10):2131-5.
[2] Li JJ, Wang H, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11.
[3] Li JJ, Wang H, Tino JA, Robl JA, Herpin TF, Lawrence RM, Biller S, Jamil H, Ponticiello R, Chen L, Chu CH, Flynn N, Cheng D, Zhao R, Chen B, Schnur D, Obermeier MT, Sasseville V, Padmanabha R, Pike K, Harrity T. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. doi: 10.1016/j.bmcl.2007.03.017. Epub 2007 Mar 12. PMID: 17383874.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3568 mL
- 11.7842 mL
- 23.5684 mL
- 5 mM
- 0.4714 mL
- 2.3568 mL
- 4.7137 mL
- 10 mM
- 0.2357 mL
- 1.1784 mL
- 2.3568 mL

技术信息

CAS号

943962-47-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H15Cl2NO4S

运输

蓝冰

分子量

424.30

别名

BMS-303141

溶解度

DMSO	85.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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