|(2-(3,5-二叔丁基-4-羟基苯基)乙烯-1,1-二基)双(膦酸)四乙酯|CsnPharm

CAS No.: 126411-39-0

SR12813 Catalog No. CSN19036

Synonyms: GW 485801

SR-12813 is a pregnane X receptor (PXR) agonist and HMG-CoA reductase inhibitor with an IC50 of 850 nM.

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生物活性

实验方案

技术信息

生物活性

描述The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase catalyzes the conversion of HMG-CoA to mevalonate, a four-electron oxidoreduction that is the rate-limiting step in the synthesis of cholesterol and other isoprenoids^[3]. SR-12813 inhibits cholesterol biosynthesis in Hep G2 cells via an enhanced degradation of HMG-CoA reductase. After 7 days plasma cholesterol was decreased by 15% in the 10 mg/kg/day group and by 19% in the 25 mg/kg/day group^[4]. SR-12813 inhibited incorporation of tritiated water into cholesterol with an IC50 of 1.2 mM but had no effect on fatty acid synthesis. Furthermore, SR-12813 reduced cellular HMG-CoA reductase activity with an IC50 of 0.85 mM. The inhibition of HMG-CoA reductase activity was rapid with a T1/2 of 10 min. After a 16-h incubation with SR-12813, mRNA levels of HMG-CoA reductase and low density lipoprotein (LDL) receptor were increased. The increased expression of LDL receptor translated into a higher LDL uptake, which can explain the primary hypocholesterolemic effect of SR-12813 in vivo^[5]. Treatment of hCMEC/D3 cells for 72 hr with rifampin or SR12813 (two well-established hPXR ligands) or PIs (atazanavir or ritonavir) resulted in an increase in P-gp expression by 1.8-, 6-, and 2-fold, respectively, with no effect observed for MRP1 expression^[6]. Preactivation of hPXR by SR12813 in MDA-MB-231 cells led to an increased resistance to Taxol at concentrations of 20 and 50 nM^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9820 mL
- 9.9101 mL
- 19.8203 mL
- 5 mM
- 0.3964 mL
- 1.9820 mL
- 3.9641 mL
- 10 mM
- 0.1982 mL
- 0.9910 mL
- 1.9820 mL

技术信息

CAS号

126411-39-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H42O7P2

运输

蓝冰

分子量

504.53

别名

GW 485801

溶解度

DMSO	100.0 mg/mL (198.2 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (198.2 mM)

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