中文名 | SR12813 |
英文名 | Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate SRL HTMT dimaleate 1ilh 4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol |
别名 | 化合物SR-12813 (2-(3,5-二叔丁基-4-羟基苯基)乙烯-1,1-二基)双(膦酸)四乙酯 |
英文别名 | SRL 1ilh SR12813 SR 12813 SR-12813 GW485801 GW 485801 GW-485801 HTMT dimaleate SR-12813(GW 485801) 4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate [[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-phosphonicacidtetraethylester Phosphonic acid, P,P'-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-, P,P,P',P'-tetraethyl ester |
CAS | 126411-39-0 |
化学式 | C24H42O7P2 |
分子量 | 504.53 |
熔点 | 119-121℃ |
溶解度 | DMSO: ≥ 10 mg/mL |
存储条件 | Sealed in dry,Room Temperature |
外观 | 固体 |
靶点 | IC50: 0.85 μM (HMG-CoA Reductase) |
体外研究 | SR12813是一种非常有效的人源和兔源PXR的激活剂,EC50分别为200 nM和700 nM。而对大鼠和小鼠PXR的激活作用非常微弱。SR-12813抑制氚化水整合到胆固醇中,IC50为1.2 μM,但对脂肪酸合成没有作用。SR-12813降低胞内HMG-CoA还原酶活性,IC50为0.85 μM,它对HMG-CoA还原酶活性的抑制非常迅速,T1/2=10 min。 |
体内研究 | SR12813在很多动物如大鼠、狗和灵长类中能够降低胆固醇水平。 |
WGK Germany | 3 |
海关编号 | 29319090 |
参考资料 展开查看 | 1. Berkhout T, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.2. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.3. Sergio C Chai, et al. Small-molecule modulators of PXR and CAR. Biochim Biophys Acta.2016 Sep;1859(9):1141-1154. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.982 ml | 9.91 ml | 19.82 ml |
5 mM | 0.396 ml | 1.982 ml | 3.964 ml |
10 mM | 0.198 ml | 0.991 ml | 1.982 ml |
5 mM | 0.04 ml | 0.198 ml | 0.396 ml |
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