S87464 |
BMS-303141 |
源叶(MedMol) | 98% |
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- 产品描述: BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 of 0.13 Μm
- 靶点: IC50: 0.13 uM (ACL);ATPCitrateLyase
- 体外研究:
In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8 μM. BMS-303141 shows no cytotoxicity up to 50 lM under a cell based Alamar Blue cytotoxicity assay, indicating the observed inhibition of lipid synthesis is not a result of compound-induced cytotoxicity.
- 体内研究:
Chronic oral dosing of BMS-303141 in high-fat fed mice lowers approximate 20-30% plasma cholesterol and triglycerides, as well as 30-50% fasting plasma glucose. Chronic treatment with BMS-303141 shows a gradual inhibition of weight gain along with a reduction in adiposity without apparent changes in food intake. BMS-303141 shows an oral bioavailability of 55% but a relatively short half-life of 2.1 h.
- 参考文献:
1. Li JJ, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.357 ml 11.784 ml 23.568 ml 5 mM 0.471 ml 2.357 ml 4.714 ml 10 mM 0.236 ml 1.178 ml 2.357 ml 50 mM 0.047 ml 0.236 ml 0.471 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)