Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Anacetrapib (MK-0859) 是 CETP 的抑制剂,能够抑制 rhCETP (IC50:7.9±2.5 nM) 和 C13S CETP 突变型 (IC50:11.8±1.9 nM) 的活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 662 | 现货 | ||
10 mg | ¥ 1,060 | 现货 | ||
25 mg | ¥ 1,960 | 现货 | ||
50 mg | ¥ 3,150 | 现货 | ||
100 mg | ¥ 4,580 | 现货 | ||
500 mg | ¥ 9,560 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 929 | 现货 |
产品描述 | Anacetrapib (MK-0859) (MK0859) is an effective, specific, reversible rhCETP and mutant CETP(C13S) inhibitor (IC50: 7.9 nM and 11.8 nM). Anacetrapib reduces the transfer of cholesteryl ester from HDL to LDL and/or VLDL thereby, producing an increase in serum HDL-cholesterol levels and a decrease in serum LDL-cholesterol levels. |
靶点活性 | CETP (recombinant human):7.9 nM, CETP (mutant, C13S):11.8 nM |
体外活性 | Anacetrapib对巨噬细胞胆固醇逆向转运有促进作用,可增加30%的排泄物胆固醇含量.处理异常仓鼠模型,持续处理2周,与对照组相比,Anacetrapib (60 mg/kg/day)使CETP活性下降94%,HDL-胆固醇上升47%,不影响非HDL胆固醇浓度.与对照组相比,Anacetrapib处理的仓鼠HDL显示ABCG1和SR-B1调节的流出物增多. [14C]Anacetrapib(10 mg/kg,p.o.)给药48 h后,鼠和猴分别恢复~80和90%放射性,但排泄物中放射性几乎无变化. |
体内活性 | Anacetrapib和抑制素联用时,既可提高HDL-胆固醇水平,也可降低LDL-胆固醇水平。Anacetrapib剂量依赖性地抑制CE从HDL3转变为HDL2。Anacetrapib对[14C]-dalcetrapibthiol与人类重组CETP的结合数无影响。 |
激酶实验 | The inhibitory potency (IC50) of Dalcetrapib, Torcetrapib, and Anacetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 μg/mL) and biotinylated LDL acceptor particles for 3 h at 37°C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting[1]. |
细胞实验 | Anacetrapib (ANA) is dissolved in DMSO and diluted with appropriate media[2]. Cells are seeded in a 96 well plate overnight prior to the treatment by different concentrations of CETP inhibitors (e.g., Anacetrapib) for 24 h. Cell viability is measured using the CellTiter-Glo Luminescent Cell Viability Assay kit. Four wells are evaluated under each experimental condition[2]. |
别名 | 安塞曲匹, MK-0859 |
分子量 | 637.51 |
分子式 | C30H25F10NO3 |
CAS No. | 875446-37-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (78.43 mM)
Ethanol: 57 mg/mL(89.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.5686 mL | 7.843 mL | 15.686 mL | 39.2151 mL |
5 mM | 0.3137 mL | 1.5686 mL | 3.1372 mL | 7.843 mL | |
10 mM | 0.1569 mL | 0.7843 mL | 1.5686 mL | 3.9215 mL | |
20 mM | 0.0784 mL | 0.3922 mL | 0.7843 mL | 1.9608 mL | |
50 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7843 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。
Anacetrapib 875446-37-0 Metabolism CETP Cholesteryl ester transfer protein inhibit Inhibitor MK0859 安塞曲匹 MK-0859 MK 0859 inhibitor