Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ertiprotafib is a PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist inhibitor ( IC50s: 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,570 | 5日内发货 | ||
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | Ertiprotafib is a PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist inhibitor ( IC50s: 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ). |
靶点活性 | PTP1B:1.6 μM, PPARβ:~1 μM (EC50), PPARα:~1 μM (EC50), IKKβ:400 nM |
体外活性 | Ertiprotafib is a potent IKK-β inhibitor (IC50: 400 nM), which is much lower than that required for the half-maximal inhibition of the p-nitrophenyl phosphatase activity of PTP1B. Ertiprotafib is at least a dual PPARα and PPARβ agonist with EC50 values for transactivation of 1 μM. The reported IC50 value of Ertiprotafib against PTP1B ranges from 1.6 to 29 μM depending on the assay conditions [2]. Such activities readily explain the observations with suprapharmacologic doses of these [1]. |
体内活性 | As seen with the treatment of ob/ob mice, both Ertiprotafib and compound 3 seem to obviously improve glucose metabolism in rats. Both Ertiprotafib and compound 3 increase in glucose disposal after an oral challenge. It is noteworthy that lipid levels are also reduced in treated animals. At 25 mg/kg/day, these compounds reduce both fasting blood glucose and insulin levels compared with vehicle-treated rats. Both triglyceride and free fatty acid levels are substantially reduced in rats treated with 25 mg/kg/day of either compound. Decreased lipid levels may be unexpected for a pure PTP1b inhibitor. As mentioned above, that rats treated with suprapharmacologic doses of Ertiprotafib display signs of PPAR family activation [2]. |
别名 | PTP 112 |
分子量 | 559.51 |
分子式 | C31H27BrO3S |
CAS No. | 251303-04-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ertiprotafib 251303-04-5 DNA Damage/DNA Repair Metabolism Phosphatase PPAR PTP-112 PTP 112 PTP112 Inhibitor inhibitor inhibit