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BMS-303141

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Chemical Structure| 943962-47-8 同义名 : -
CAS号 : 943962-47-8
货号 : A169881
分子式 : C19H15Cl2NO4S
纯度 : 99%+
分子量 : 424.298
MDL号 : MFCD25976797
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(58.92 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.57mL

4.71mL

2.36mL
参考文献

[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.