| 名称 | Anacetrapib |
| 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. |
| 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]. |
| 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]. |
| 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。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (78.43 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2.5 mg/mL (3.92 mM), Sonication is recommeded.
Ethanol : 57 mg/mL (89.41 mM), Sonication is recommended.
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| 关键字 | rhCETP | Mutant CETP (C13S) | MK0859 | MK 0859 | Inhibitor | inhibit | Cholesteryl ester transfer protein | CETP | Anacetrapib |
| 相关产品 | Dalcetrapib | 3-Pyridinemethanol | Obicetrapib | 20-HC-Me-Pyrrolidine | BMS-188494 | Torcetrapib | Azacosterol hydrochloride | CP-532623 | Implitapide | BMS-795311 | Evacetrapib | CKD-519 |
| 相关库 | 抑制剂库 | 脂代谢化合物库 | 经典已知活性库 | 已知活性化合物库 | ReFRAME 相关化合物库 | 含氟化合物库 | 抗心血管疾病化合物库 | 抗肥胖化合物库 | 临床期小分子药物库 | 药物功能重定位化合物库 | 抗代谢疾病化合物库 | 表型筛选靶点鉴定库 |