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SR12813
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SR12813图片
CAS NO:126411-39-0
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
GW 485801
SR-12813
SR 12813
产品介绍
SR12813 是一种人孕烷X受体激动剂,还是一种 3-羟基-3-甲基-戊二酰辅酶 A 还原酶抑制剂,IC50值为 0.85 μM。

产品描述

SR-12813 is a pregnane X receptor (PXR) agonist.

体外活性

SR12813 is a very potent and efficacious activator of both the human and rabbit PXR, with EC50 values of approximately 200 nM and 700 nM, respectively. By contrast, SR12813 is only a very weak activator of the rat and mouse PXR[1]. SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 μM but has no effect on fatty acid synthesis. SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 μM. The inhibition of HMG-CoA reductase activity is rapid with a T1/2 of 10 min[2].

体内活性

The bisphosphonate ester SR12813 lowers cholesterol levels in a range of species including rats, dogs and primates[1].

激酶实验

Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cells are lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassium dihydrophosphate, 30 mM EDTA, 5 mM dithiothreitol, pH 7.4 at room temperature. In some experiments KF is omitted to measure "total" HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate is further determined.

细胞实验

Hep G2 cells are incubated for 21 h with either 1 μM lovastatin or 3 μM SR-12813 in 5% LPDS medium. mRNA is isolated and analyzed by Northern blotting.(Only for Reference)

Cas No.

126411-39-0

分子式

C24H42O7P2

分子量

504.541

别名

GW 485801;SR-12813;SR 12813

储存和溶解度

Ethanol:50.5 mg/mL (100 mM)
DMSO:50.5 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years