BMS-309403
Cat. No.:YN370212
产品名称: | BMS-309403 |
CAS No.: | 300657-03-8 |
Chemical Name: | 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-acetic acid |
Synonyms: | BMS 309403,BMS309403 |
分子量: | 474.55 |
分子式: | C₃₁H₂₆N₂O₃ |
SMILES: | O=C(O)COC1=CC(C2=CC=CC=C2N3N=C(C4=CC=CC=C4)C(C5=CC=CC=C5)=C3CC)=CC=C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | BMS-309403 是一种有效的,选择性的,细胞可渗透性的脂肪细胞脂肪酸结合蛋白(FABP4)抑制剂,Ki值小于 2 nM。BMS-309403 对 FABP3 的 Ki值为 250 nM,对 FABP5 的 Ki值为 350 nM。BMS-309403 与蛋白质内部的脂肪酸结合囊相互作用,竞争性地抑制内源性脂肪酸的结合。 |
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Lan, H., Cheng, C.C., Kowalski, T.J., et al.Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesityJ. Lipid Res.52(4),646-656(2011)
Sulsky, R., Magnin, D.R., Huang, Y., et al.Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP)Bioorg. Med. Chem. Lett.17(12),3511-3515(2007)
Furuhashi, M., Tuncman, G., Görgün, C.Z., et al.Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2Nature447,959-965(2007)
Lee, M.Y., Li, H., Xiao, Y., et al.Chronic administration of BMS309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cellsBr. J. Pharmacol.162(7),1564-1576(2011)
Suhre, K., Römisch-Margl, W., de Angelis, M.H., et al.Identification of a potential biomarker for FABP4 inhibition: The power of lipidomics in preclinical drug testingJ. Biomol. Screen.16(5),467-475(2011)