24136-23-0
基本信息
4-氯-ALPHA-[3-(三氟甲基)苯氧基]苯乙酸 2-(乙酰基氨基)乙酯
JNJ 39659100
Arhalofenate
MBX-102 >=98% (HPLC)
4-Chloro-alpha-[3-(trifluoromethyl)phenoxy]benzeneacetic acid 2-(acetylamino)ethyl ester
(aR)-4-Chloro-a-[3-(trifluoromethyl)phenoxy]benzeneacetic acid 2-(acetylamino)ethyl ester
Benzeneaceticacid,4-chloro-α-[3-(trifluoromethyl)phenoxy]-,2-(acetylamino)ethylester,(αR)-
Benzeneacetic acid, 4-chloro-α-[3-(trifluoromethyl)phenoxy]-, 2-(acetylamino)ethyl ester, (αR)-
物理化学性质
| 沸点 | 551.1±50.0 °C(Predicted) |
| 密度 | 1.331 |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥35mg/mL |
| 酸度系数(pKa) | 15.32±0.46(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至棕褐色 |
安全数据
| 危险性符号(GHS) |   GHS06,GHS09 |
| 警示词 | 危险 |
| 危险性描述 | H301-H319-H400 |
| 防范说明 | P273-P301+P310+P330-P305+P351+P338 |
| 危险品标志 | T,N |
| 危险类别码 | 25-36-50/53 |
| 安全说明 | 26-45-60-61 |
| 危险品运输编号 | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
常见问题列表
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PPAR-γ
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Arhalofenate (MBX 102) is a prodrug ester, that is rapidly and completely modified in vivo by non-specific serum esterases to the mature free acid form Arhalofenate (MBX 102) acid. Arhalofenate (MBX 102) shows a dose-dependent activation of mouse GAL4-PPAR-γ with EC 50 s of appr 12 μM.
Arhalofenate (MBX 102) (100 mg/kg, p.o.) significantly increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (MBX 102) (60 mg/kg) leads to a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels. Arhalofenate (MBX 102) (100 mg/kg, p.o.) significantly decreases triglyceride, free fatty acid, and cholesterol levels in ZDF rats. MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (MBX 102) (100 mg/kg, p.o.) also significantly lowers fasting plasma insulin, and robustly decreases fasting plasma triglycerides after 32 days of treatment in Zucker Fatty (ZF) rats.