- 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.
