CAS NO: | 126411-39-0 |
生物活性 | SR12813 (GW 485801) is an inhibitor of3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50value of 0.85 μM[1][2]. SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR)[3]. | ||||||||||||||||
IC50& Target | IC50: 0.85 μM (HMG-CoA Reductase) | ||||||||||||||||
体外研究 (In Vitro) | SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50of 1.2 μM but has no effect on fatty acid synthesis. Furthermore, SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50of 0.85 μM[1]. Both 25-HC and SR-12813 can kill mammalian cells through blocking the synthesis of cholesterol, thereby they are ideal regents for lethal selection. SR-12813 kills HeLa cells at concentration range from 8 μM to 16 μM. SR-12813 kills wild type cells and mutant cells infected by Ad-Cre (SL-5+Cre), but the mutant SL-5 survives this condition. SR-12813 or 25-HC promotes the degradation of the 95-KDa full-length HMG-CoA reductase in wild type HeLa and SL-5 mutant cells[1]. | ||||||||||||||||
分子量 | 504.53 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H42O7P2 | ||||||||||||||||
CAS 号 | 126411-39-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(99.10 mM) *"≥" means soluble, but saturation unknown. 配制储备液
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以下溶剂前显示的百
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