Anacetrapib, also known as MK-0859, is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.
仅供研究使用。 我们不向患者出售。
名称 | Anacetrapib |
---|---|
Iupac 化学名称 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-((4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methyl)-4-methyloxazolidin-2-one. |
同义词 | MK0859; MK-0859; MK 0859; Anacetrapib |
英文同义词 | MK0859; MK-0859; MK 0859; Anacetrapib |
分子式 | C30H25F10NO3 |
分子量 | 637.51 |
Smile | O=C1O[C@H](C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)[C@H](C)N1CC3=CC(C(F)(F)F)=CC=C3C4=CC(C(C)C)=C(F)C=C4OC |
InChiKey | MZZLGJHLQGUVPN-HAWMADMCSA-N |
InChi | InChI=1S/C30H25F10NO3/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40/h5-12,14-15,26H,13H2,1-4H3/t15-,26-/m0/s1 |
Cas号 | 875446-37-0 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
---|---|---|---|---|
大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
---|---|
纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 可溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
海关编码 |
Targets | |
---|---|
Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Krishna R, Stypinski D, Ali M, Garg A, Cote J, Maes A, Degroot B, Liu Y, Li S, Connolly SM, Wagner JA, Stoch SA. Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects. Br J Clin Pharmacol. 2012 Jul;74(1):116-24. doi: 10.1111/j.1365-2125.2012.04171.x. PubMed PMID: 22243494.
2: Hooper AJ, Burnett JR. Anacetrapib, a cholesteryl ester transfer protein inhibitor. Expert Opin Investig Drugs. 2012 Jan;21(1):103-9. Epub 2011 Dec 22. PubMed PMID: 22191425.
3: Krauss RM, Wojnooski K, Orr J, Geaney JC, Pinto CA, Liu Y, Wagner JA, Luk JM, Johnson-Levonas AO, Anderson MS, Dansky HM. Changes in lipoprotein subfraction concentration and composition in healthy individuals treated with the CETP inhibitor anacetrapib. J Lipid Res. 2012 Mar;53(3):540-7. Epub 2011 Dec 17. PubMed PMID: 22180633; PubMed Central PMCID: PMC3276477.
4: Gutstein DE, Krishna R, Johns D, Surks HK, Dansky HM, Shah S, Mitchel YB, Arena J, Wagner JA. Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction. Clin Pharmacol Ther. 2012 Jan;91(1):109-22. doi: 10.1038/clpt.2011.271. Epub 2011 Nov 30. Review. PubMed PMID: 22130116.
5: Aperis G, Paliouras C, Tsampikaki E, Papakonstantinou N, Alivanis P. Anacetrapib: a new weapon against dyslipidemia. Curr Clin Pharmacol. 2011 Nov;6(4):227-35. Review. PubMed PMID: 22082322.
6: Krishna R, Stypinski D, Ali M, Garg A, Gendrano IN 3rd, Maes A, DeGroot B, Liu Y, Li S, Connolly SM, Wagner JA, Stoch SA. Lack of an effect of anacetrapib on the pharmacokinetics of digoxin in healthy subjects. Biopharm Drug Dispos. 2011 Dec;32(9):525-9. doi: 10.1002/bdd.776. PubMed PMID: 22031172.
7: Dansky HM, Bloomfield D, Gibbons P, Liu S, Sisk CM, Tribble D, McKenney JM, Littlejohn TW 3rd, Mitchel Y. Efficacy and safety after cessation of treatment with the cholesteryl ester transfer protein inhibitor anacetrapib (MK-0859) in patients with primary hypercholesterolemia or mixed hyperlipidemia. Am Heart J. 2011 Oct;162(4):708-16. Epub 2011 Sep 1. PubMed PMID: 21982664.
8: Castro-Perez J, Briand F, Gagen K, Wang SP, Chen Y, McLaren DG, Shah V, Vreeken RJ, Hankemeier T, Sulpice T, Roddy TP, Hubbard BK, Johns DG. Anacetrapib promotes reverse cholesterol transport and bulk cholesterol excretion in Syrian golden hamsters. J Lipid Res. 2011 Nov;52(11):1965-73. Epub 2011 Aug 14. PubMed PMID: 21841206; PubMed Central PMCID: PMC3196228.
9: Smith CJ, Ali A, Hammond ML, Li H, Lu Z, Napolitano J, Taylor GE, Thompson CF, Anderson MS, Chen Y, Eveland SS, Guo Q, Hyland SA, Milot DP, Sparrow CP, Wright SD, Cumiskey AM, Latham M, Peterson LB, Rosa R, Pivnichny JV, Tong X, Xu SS, Sinclair PJ. Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib. J Med Chem. 2011 Jul 14;54(13):4880-95. Epub 2011 Jun 17. PubMed PMID: 21682257.
10: Jialal I, Kaur J. The cholesterol ester transfer protein inhibitor, anacetrapib. Curr Opin Lipidol. 2011 Jun;22(3):245-6. Erratum in: Curr Opin Lipidol. 2011 Aug;22(4):326. PubMed PMID: 21562390.