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251303-04-5

中文名称 ERTIPROTAFIB
英文名称 Ertiprotafib
CAS 251303-04-5
分子式 C31H27BrO3S
分子量 559.51
MOL 文件 251303-04-5.mol
更新日期 2023/03/20 19:56:43
251303-04-5 结构式 251303-04-5 结构式

基本信息

中文别名
化合物 T15243
英文别名
PTP 112
Ertiprotafib
Benzenepropanoic acid, a-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-,(aR)-
Benzenepropanoic acid, α-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-, (αR)-
所属类别
生物化工:抑制剂

物理化学性质

沸点690.7±55.0 °C(Predicted)
密度1.376±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)3.21±0.10(Predicted)

常见问题列表

生物活性
Ertiprotafib 是 PTP1B, IKK-β 的抑制剂,其 IC50 值分别是 1.6 μM,400 nM,同时也是PPARα/PPARβ 的激动剂,其 EC50 值为 ~1 μM。
靶点

PTP1B

1.6 μM (IC 50 )

IKK-β

400 nM (IC 50 )

PPARα

~1 μM (EC 50 )

PPARβ

~1 μM (EC 50 )

体外研究

Ertiprotafib is a potent inhibitor of IKK-β, with an IC 50 value of 400±40 nM, which is much lower than that required for the half-maximal inhibition of the p-nitrophenyl phosphatase activity of PTP1B. The reported IC 50 value of Ertiprotafib against PTP1B ranges from 1.6 to 29 μM depending on the assay conditions. Ertiprotafib is at least a dual PPARα and PPARβ agonist with EC 50 values for transactivation of 1 μM. Such activities readily explain the observations with suprapharmacologic doses of these.

体内研究

As seen with treatment of ob/ob mice, both Ertiprotafib and compound 3 seem to significantly improve glucose metabolism in rats. At 25 mg/kg/day, these compounds decrease both fasting blood glucose and insulin levels compared with vehicle treated rats. Furthermore, both Ertiprotafib and compound 3 increase glucose disposal after an oral challenge. It is noteworthy that lipid levels are also reduced in treated animals. Both triglyceride and free fatty acid levels are substantially reduced in rats treated with 25 mg/kg/day of either compound. To summarize, both Ertiprotafib and compound 3 seem to be robust agents in improving glucose utilization in fa/fa rats while also decreasing lipid levels in these animals. Decreased lipid levels may be unexpected for a pure PTP1b inhibitor. It is more telling, as mentioned above, that rats treated with suprapharmacologic doses of Ertiprotafib show signs of PPAR family activation.

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