Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SR12813 (GW 485801) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 195 | 现货 | ||
5 mg | ¥ 410 | 现货 | ||
10 mg | ¥ 623 | 现货 | ||
25 mg | ¥ 1,176 | 现货 | ||
50 mg | ¥ 1,767 | 现货 | ||
100 mg | ¥ 2,653 | 现货 | ||
200 mg | ¥ 3,983 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 464 | 现货 |
产品描述 | SR12813 (GW 485801) is a pregnane X receptor (PXR) agonist. |
靶点活性 | HMG-CoA reductase:850 nM |
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) |
别名 | SR-12813, SR 12813, GW 485801 |
分子量 | 504.53 |
分子式 | C24H42O7P2 |
CAS No. | 126411-39-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50.5 mg/mL (100 mM)
Ethanol: 50.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.982 mL | 9.9102 mL | 19.8204 mL | 49.5511 mL |
5 mM | 0.3964 mL | 1.982 mL | 3.9641 mL | 9.9102 mL | |
10 mM | 0.1982 mL | 0.991 mL | 1.982 mL | 4.9551 mL | |
20 mM | 0.0991 mL | 0.4955 mL | 0.991 mL | 2.4776 mL | |
50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.991 mL | |
100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SR12813 126411-39-0 Autophagy Metabolism HMG-CoA Reductase GW-485801 SR-12813 HMG-CoA Reductase (HMGCR) inhibit Inhibitor GW485801 SR 12813 GW 485801 inhibitor