切换导航

Anacetrapib (MK-0859)

现货
Catalog No.
A4375
RhCETP/突变型 CETP(C13S) 抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,700.00
现货
5mg
¥ 1,200.00
现货
10mg
¥ 2,000.00
现货
50mg
¥ 5,800.00
现货
200mg
¥ 14,800.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Anacetrapib, also known as MK-0859, is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) that exhibits strong inhibition against CETP-mediated transfer of cholesteryl esters and triglycerides with values of inhibition constant IC50 of 16 nM and 29 nM respectively. Anacetrapib is mainly metabolized by CYP3A4 through O-demethylation, hydroxylation on the biphenyl moiety and hydroxylation on the isopropyl side chain resulting in three oxidative metabolites M1, M2 and M3 respectively. Anacetrapib is being investigated for the treatment of primary hypercholesterolemia and mixed hyperlipidemia due to its impressive effects to lower low-density lipoprotein (LDL) cholesterol levels and increase high-density lipoprotein (HDL) cholesterol levels without any associated major adverse events.

Reference

Tan EY, Hartmann G, Chen Q, Pereira A, Bradley S, Doss G, Zhang AS, Ho JZ, Braun MP, Dean DC, Tang W, Kumar S. Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys. Drug Metab Dispos. 2010;38(3):459-473.

Kumar S, Tan EY, Hartmann G, Biddle Z, Bergman AJ, Dru J, Ho JZ, Jones AN, Staskiewicz SJ, Braun MP, Karanam B, Dean DC, Gendrano IN, Graves MW, Wagner JA, Krishna R. Metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans. Drug Metab Dispos. 2010;38(3):474-483

文献引用

1. Lee EY, Yoo JA, et al. "Anti-Aging and Tissue Regeneration Ability of Policosanol Along with Lipid-Lowering Effect in Hyperlipidemic Zebrafish via Enhancement of High-Density Lipoprotein Functionality." Rejuvenation Res. 2016 Apr;19(2):149-58. PMID:26413884

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt637.51
Cas No.875446-37-0
FormulaC30H25F10NO3
SynonymsMK 0859, MK0859
Solubility≥31.9 mg/mL in DMSO, ≥86.6 mg/mL in EtOH, <2.23 mg/mL in H2O
Chemical Name(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-oxazolidin-2-one
SDFDownload SDF
Canonical SMILESCC1C(OC(=O)N1CC2=C(C=CC(=C2)C(F)(F)F)C3=CC(=C(C=C3OC)F)C(C)C)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Description Anacetrapib是一种有效的、选择性的和可逆的rhCETP和突变 CETP(C13S)抑制剂,IC50值分别为7.9 nM和11.8 nM。
靶点 rhCETP mutant CETP(C13S)        
IC50 7.9 nM 11.8 nM        

质量控制

化学结构

Anacetrapib (MK-0859)

相关生物数据

Anacetrapib (MK-0859)