Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RP-64477 是有效的胆固醇酯化酶酰基辅酶 A:胆固醇 O-酰基转移酶 (ACAT) 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 739 | 现货 | ||
5 mg | ¥ 1,830 | 现货 | ||
10 mg | ¥ 2,960 | 现货 | ||
25 mg | ¥ 4,880 | 现货 | ||
50 mg | ¥ 6,990 | 现货 | ||
100 mg | ¥ 9,430 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,990 | 现货 |
产品描述 | RP-64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor. |
体内活性 | Inhibition by RP 64477 in a rabbit intestinal enzyme preparation was shown to be non-competitive with respect to the substrate oleoyl-CoA. In whole cell assays using human intestinal (CaCo-2), hepatic HepG2) and monocytic (THP-1) cell lines, RP 64477 inhibited ACAT activity with IC50s of 113, 503, and 180 nM, respectively. RP 64477 (0.03% w/w by diet) reduced significantly cholesterol absorption in cholesterol/cholic acid-fed rats from 94+/- 8% to 65 +/- 4%. In cholesterol-fed rabbits, cholesterol absorption was reduced from 72 +/- 5% to 50 +/-5% and 44 +/- 5% at dose levels of 10 and 30 mg kg-1 b.i.d., respectively. Plasma cholesterol levels were reduced dose-dependently in both cholesterol/cholic-acid-fed rats and cholesterol-fed rabbits. Neither cholesterol absorption nor plasma cholesterol levels were reduced significantly in animals maintained on standard laboratory diets. Pharmacokinetic studies indicated that RP 64477 were very poorly absorbed following oral administration to rats. |
别名 | RP64477 |
分子量 | 498.72 |
分子式 | C29H42N2O3S |
CAS No. | 135239-65-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 8.33 mg/mL (16.70 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0051 mL | 10.0257 mL | 20.0513 mL | 50.1283 mL |
5 mM | 0.401 mL | 2.0051 mL | 4.0103 mL | 10.0257 mL | |
10 mM | 0.2005 mL | 1.0026 mL | 2.0051 mL | 5.0128 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。
RP-64477 135239-65-5 Metabolism Acyltransferase Diglyceride acyltransferase inhibit mono- acylglycerol acyltransferase RP64477 RP 64477 Inhibitor acyl-CoA:cholesterol acyltransferase Diacylglycerol acyltransferase inhibitor