产品描述: | SR-12813是孕烷X受体(PXR)的激动剂 |
靶点: |
pregnane X receptor; HMG-CoA reductase:850 nM;HMG-CoAReductase; Autophagy |
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 |
细胞实验: |
Cell lines: HepG2细胞 Concentrations: 3 μM Incubation Time: 21 h Method: 在5% LPDS细胞培养基中加入1 μM lovastatin或3 μM SR-12813,处理Hep G2细胞21小时,提取mRNA进行Northern blotting分析。 |
动物实验: |
Animal Models: 比格犬 Dosages: 10 mg/kg Administration: 口服 |
参考文献: |
1. Jones SA, et al. The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Mol Endocrinol. 2000, 14(1):27-39. 2. Berkhout TA, 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, 271(24):14376-82. 3. Berkhout TA, et al. SR-12813 lowers plasma cholesterol in beagle dogs by decreasing cholesterol biosynthesis. Atherosclerosis. 1997, 133(2):203-12. |
溶解性: |
Soluble in DMSO、Ethanol |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
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 |
50 mM |
0.04 ml |
0.198 ml |
0.396 ml |
|
注意: |
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