中文名 | BMS-303141 |
英文名 | BMS-303141 |
别名 | 3,5-二氯-2-羟基-N-(4-甲氧基[1,1'-联苯]-3-基)苯磺酰胺 |
英文别名 | CS-887 BMS30314 BMS303141 BMS 303141 BMS-303141 3,5-dichloro-2-hydroxy-N-(4-Methoxybiphenyl-3-yl)benzenesulfonaMide 3,5-dichloro-2-hydroxy-N-(2-methoxy-5-phenylphenyl)benzenesulfonamide 3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)benzenesulfonamide 3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1'-biphenyl]-3-yl)-benzenesulfonamide BMS 303141 |
CAS | 943962-47-8 |
化学式 | C19H15Cl2NO4S |
分子量 | 424.3 |
密度 | 1.462±0.06 g/cm3(Predicted) |
沸点 | 591.5±60.0 °C(Predicted) |
溶解度 | DMSO: 可溶20mg/mL,澄清 |
酸度系数 | 4.94±0.48(Predicted) |
存储条件 | 2-8°C |
稳定性 | 从提供的购买之日起稳定2年。DMSO或乙醇中的溶液可以在-20 °C下储存长达3个月。 |
外观 | 粉末 |
颜色 | white to beige |
靶点 | ACL |
体外研究 | In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC 50 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. |
WGK Germany | 3 |
参考资料 展开查看 | 1: Guo Q, Kang H, Wang J, Dong Y, Peng R, Zhao H, Wu W, Guan H, Li F. Inhibition of ACLY Leads to Suppression of Osteoclast Differentiation and Function Via Regulation of Histone Acetylation. J Bone Miner Res. 2021 Jun 22. doi: 10.1002/jbmr.4399. Epub ahead of print. PMID: 34155695. 2: Zheng Y, Zhou Q, Zhao C, Li J, Yu Z, Zhu Q. ATP citrate lyase inhibitor triggers endoplasmic reticulum stress to induce hepatocellular carcinoma cell apoptosis via p-eIF2α/ATF4/CHOP axis. J Cell Mol Med. 2021 Feb;25(3):1468-1479. doi: 10.1111/jcmm.16235. Epub 2021 Jan 3. PMID: 33393219; PMCID: PMC7875901. 3: Vaughn N, Haviland DL. Acly promotes metabolic reprogramming and induction of IRF4 during early CD8+ T cell activation. Cytometry A. 2021 Aug;99(8):825-831. doi: 10.1002/cyto.a.24294. Epub 2020 Dec 29. PMID: 33325591. |
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 |
5 mM | 0.047 ml | 0.236 ml | 0.471 ml |
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