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BMS309403 |
| CAS No.: |
300657-03-8 |
| 分子式： |
C31H26N2O3 |
| 分子量： |
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| 备注： |
中文名称BMS309403中文同义词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;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;化合物BMS-309403;INHIBITOR|||BMS309403|||SELECTIVE|||BMS309403|||BMS-309403|||ORAL|||FATTYACID-BINDINGPROTEIN|||INHIBIT|||BMS-309403|||BMS309403|||ENDOTHELIAL|||UPTAKE|||GLUCOSE|||FABP|||BMS309403|||FUNCTION英文名称2’’-(5-ETHYL-3,4-DIPHENYL-PYRAZOL-1-YL)-BIPHENYL-3-YLOXY]ACETICACID英文同义词2’’-(5-ETHYL-3,4-DIPHENYL-PYRAZOL-1-YL)-BIPHENYL-3-YLOXY]ACETICACID;2-[[2’-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1’-biphenyl]-3-yl]oxy]-aceticacid;BMS309403;3-[2-(5-ETHYL-3,4-DIPHENYLPYRAZOL-1-YL)PHENYL]PHENOXYACETICACID;CS-495;BMS309403;BMS309403;Aceticacid,2-[[2’-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1’-biphenyl]-3-yl]oxy]-;2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]aceticacidCAS号300657-03-8分子式C31H26N2O3分子量474.55EINECS号相关类别试剂;FABP4Inhibitor;selectiveinhibitorofadiChemicalbookpocyteFatty-Acid-BindingProtein(aFABP/aP2)Mol文件300657-03-8.mol结构式BMS309403性质沸点657.5±55.0°C(Predicted)密度1.17储存条件Sealedindry,RoomTemperature溶解度可溶于DMSO（高达至少25mg/ml）。形态白色粉末状固体。酸度系数(pKa)3.15±0.10(Predicted)颜色灰白色或浅黄色稳定性可在-20°下的DMSO中的溶液储存长达1个月。BMS309403用途与合成方法生物活性BMS309403是FABP4小分子抑制剂，Kd值为4nM，对FABP4的选择性比对FABP5和FABP3高100倍以上。靶点TargetValueFABP4(Cell-freeassay)4nM(Kd)体外研究TreatmentwithBMS-309403significantlydecreasedMCP-1productionfromTHP-1macrophagesinadose-andtime-dependentmanner.体内研究BMS-309403sodium(15mg/kg;chronictreatment;dailyfor6weeks)improvesendothelialfunction,phosphorylatedandtotaleNOSandreducedplasmatriglyceridelevelsbutdidnotaffectendothelium-independentrelaxations.AnimalModel:C57BL/6Jmice(ApoE−/−mice)Dosage:15mg/kgAdministration:Chronictreatment;dailyfor6weeksResult:SignificantlyincreasedthephosphorylatedeNOS(Ser1177)andtotaleNOSbutnotthephosphorylatedtototaleNOSratioinaortaeof18weeksoldApoE−/−mice. |
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