300657-03-8 2-[[2'-(5-乙基-3,4-二苯基-1H-吡唑-1-基)[1,1'-联苯]-3-基]氧基]乙酸

中文名称: 2-[[2'-(5-乙基-3,4-二苯基-1H-吡唑-1-基)[1,1'-联苯]-3-基]氧基]乙酸
英文名称: 2-((2'-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)-[1,1'-biphenyl]-3-yl)oxy)acetic acid
CAS号

词条详情加载中…

名称和标识

中文名: 2-[[2'-(5-乙基-3,4-二苯基-1H-吡唑-1-基)[1,1'-联苯]-3-基]氧基]乙酸
英文名: 2-((2'-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)-[1,1'-biphenyl]-3-yl)oxy)acetic acid
CAS号: 300657-03-8
分子式: C31H26N2O3
分子量: 474.55
中文别名: 2-(5-乙基-3,4-二苯基-吡唑-1-基)-联苯-3-基氧基]乙酸; 2'-(5-乙基-3,4-二苯基-吡唑-1-基)-双苯基-3-氧基]乙酸; BMS309403; BMS-309403; BMS 309403; 化合物BMS-309403; BMS-309403抑制剂
英文别名: 2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid; 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]acetic acid; 3-[2-(5-ETHYL-3,4-DIPHENYLPYRAZOL-1-YL)PHENYL]PHENOXYACETIC ACID; Acetic acid, 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-; {[2'-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)-3-biphenylyl]oxy}acetic acid; ((2'-(5-Ethyl-3,4-Diphenyl-1h-Pyrazol-1-Yl)-3-Biphenylyl)oxy)acetic Acid; [2'-(5-Ethyl-3,4-diphenyl-pyrazol-1-yl)-biphenyl-3-yloxy]acetic acid; BMS309403; BMS 309403; BMS-309403

安全说明

危险性质：非危险化学品

用途与制备

生物活性 BMS309403是FABP4小分子抑制剂，Kd值为4 nM，对FABP4的选择性比对FABP5和FABP3高100倍以上。
靶点 Target Value FABP4 (Cell-free assay) 4 nM(Kd)
体外研究 Treatment with BMS-309403 significantly decreased MCP-1 production from THP-1 macrophages in a dose- and time-dependent manner.
体内研究 BMS-309403 sodium (15 mg/kg; chronic treatment; daily for 6 weeks) improves endothelial function, phosphorylated and total eNOS and reduced plasma triglyceride levels but did not affect endothelium-independent relaxations. Animal Model: C57BL/6J mice (ApoE −/− mice) Dosage: 15 mg/kg Administration: Chronic treatment ; daily for 6 weeks Result: Significantly increased the phosphorylated eNOS (Ser1177) and total eNOS but not the phosphorylated to total eNOS ratio in aortae of 18 weeks old ApoE −/− mice.

医药