化合物 T15243
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- CAS号:
- 251303-04-5
- 英文名:
- Ertiprotafib
- 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)-
- 中文名:
- 化合物 T15243
- 中文别名:
- 化合物 T15243
- CBNumber:
- CB63215487
- 分子式:
- C31H27BrO3S
- 分子量:
- 559.52
- MOL File:
- 251303-04-5.mol
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化合物 T15243化学性质
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沸点:
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690.7±55.0 °C(Predicted)
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密度:
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1.376±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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3.21±0.10(Predicted)
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化合物 T15243性质、用途与生产工艺
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。
PTP1B
1.6 μM (IC
50
)
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IKK-β
400 nM (IC
50
)
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PPARα
~1 μM (EC
50
)
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PPARβ
~1 μM (EC
50
)
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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.
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.
化合物 T15243
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-19383 | Ertiprotafib | | 1 mg | 1590元 |
2024/04/30 | HY-19383 | Ertiprotafib | | 5 mg | 3500元 |
251303-04-5, 化合物 T15243 相关搜索:
- C31H27BrO3S
- 化合物 T15243
- 251303-04-5
- Benzenepropanoic acid, α-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-, (αR)-
- PTP 112
- Ertiprotafib
- Benzenepropanoic acid, a-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thien-4-yl)-2,6-dimethylphenoxy]-,(aR)-