For research use only. Not for therapeutic Use.
Anacetrapib (Cat.No:I005272) is a medication used for the treatment of high cholesterol levels. It works by inhibiting an enzyme called cholesteryl ester transfer protein (CETP) which helps to increase high-density lipoprotein (HDL) levels and decrease low-density lipoprotein (LDL) levels in the blood. Anacetrapib has been found to be effective in reducing the risk of cardiovascular events in patients with high cholesterol.
| Catalog Number | I005272 |
| CAS Number | 875446-37-0 |
| Synonyms | (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 |
| Molecular Formula | C₃₀H₂₅F₁₀NO₃ |
| Purity | ≥95% |
| Target | CETP |
| Solubility | DMSO ≥125mg/mL Water <1.2mg/mL Ethanol ≥125mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 7.9 nM/11.8 nM(rhCETP/CETP(C13S)) [1] |
| IUPAC 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 |
| 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 |
| InChIKey | MZZLGJHLQGUVPN-HAWMADMCSA-N |
| SMILES | CC1C(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 |
| Reference | </br>1:Dalcetrapib and anacetrapib differently impact HDL structure and function in rabbits and monkeys. Brodeur MR, Rhainds D, Charpentier D, Mihalache-Avram T, Mecteau M, Brand G, Chaput E, Perez A, Niesor EJ, Rhéaume E, Maugeais C, Tardif JC.J Lipid Res. 2017 May 17. pii: jlr.M068940. doi: 10.1194/jlr.M068940. [Epub ahead of print] PMID: 28515138 Free Article</br>2:Lipid-modifying efficacy and tolerability of anacetrapib added to ongoing statin therapy in Japanese patients with dyslipidemia. Teramoto T, Daida H, Ikewaki K, Arai H, Maeda Y, Nakagomi M, Shirakawa M, Watanabe Y, Kakikawa T, Numaguchi H, Johnson-Levonas AO, Blaustein RO.Atherosclerosis. 2017 Jun;261:69-77. doi: 10.1016/j.atherosclerosis.2017.03.009. Epub 2017 Mar 10. PMID: 28478132 Free Article</br>3:Randomized Evaluation of the Effects of Anacetrapib through Lipid-modification (REVEAL)-A large-scale, randomized, placebo-controlled trial of the clinical effects of anacetrapib among people with established vascular disease: Trial design, recruitment, and baseline characteristics. Landray MJ, Reveal Collaborative Group; L. Bowman, F. Chen, E. Sammons, J.C. Hopewell, K. Wallendszus, W. Stevens, E. Valdes-Marquez, S. Wiviott, C.P. Cannon, E. Braunwald, R. Collins, M.J. Landray (Writing Committtee)..Am Heart J. 2017 May;187:182-190. doi: 10.1016/j.ahj.2017.02.021. Epub 2017 Feb 21. PMID: 28454801 Free PMC Article</br>4:Anacetrapib-driven triglyceride lowering explained: The fortuitous role of CETP in the intravascular catabolism of triglyceride-rich lipoproteins. Brown AL, Brown JM.J Lipid Res. 2017 Apr 21. pii: jlr.C077131. doi: 10.1194/jlr.C077131. [Epub ahead of print] No abstract available. PMID: 28432183 Free Article</br>5:Chronic Administration of Anacetrapib Is Associated With Accumulation in Adipose and Slow Elimination. Krishna R, Gheyas F, Liu Y, Hagen DR, Walker B, Chawla A, Cote J, Blaustein RO, Gutstein DE.Clin Pharmacol Ther. 2017 Apr 5. doi: 10.1002/cpt.700. [Epub ahead of print] PMID: 28380664 </br>6:Effects of CETP Inhibition with Anacetrapib on Metabolism of VLDL TG and Plasma Apolipoproteins C-II, C-III, and E. Millar JS, Lassman ME, Thomas T, Ramakrishnan R, Jumes P, Dunbar RL, deGoma EM, Baer AL, Karmally W, Donovan DS, Rafeek H, Wagner JA, Holleran S, Obunike J, Liu Y, Aoujil S, Standiford T, Gutstein DE, Ginsberg HN, Rader DJ, Reyes-Soffer G.J Lipid Res. 2017 Mar 17. pii: jlr.M074880. doi: 10.1194/jlr.M074880. [Epub ahead of print] PMID: 28314859 Free Article</br>7:Anacetrapib, but not evacetrapib, impairs endothelial function in CETP-transgenic mice in spite of marked HDL-C increase. Simic B, Mocharla P, Crucet M, Osto E, Kratzer A, Stivala S, Kühnast S, Speer T, Doycheva P, Princen HM, van der Hoorn JW, Jukema JW, Giral H, Tailleux A, Landmesser U, Staels B, Lüscher TF.Atherosclerosis. 2017 Feb;257:186-194. doi: 10.1016/j.atherosclerosis.2017.01.011. Epub 2017 Jan 16. PMID: 28152406 </br>8:Lipid-Modifying Efficacy and Tolerability of Anacetrapib Added to Ongoing Statin Therapy in Patients with Hypercholesterolemia or Low High-Density Lipoprotein Cholesterol. Ballantyne CM, Shah S, Kher U, Hunter JA, Gill GG, Cressman MD, Ashraf TB, Johnson-Levonas AO, Mitchel YB.Am J Cardiol. 2017 Feb 1;119(3):388-396. doi: 10.1016/j.amjcard.2016.10.032. Epub 2016 Nov 1. PMID: 27956003 Free Article</br>9:Pharmacokinetic drug evaluation of anacetrapib for the treatment of dyslipidemia. Borghi C, Cicero AF.Expert Opin Drug Metab Toxicol. 2017 Feb;13(2):205-209. doi: 10.1080/17425255.2017.1262347. Epub 2016 Dec 4. Review. PMID: 27852117 </br>10:Assessment of pharmacokinetics, bioavailability and protein binding of anacetrapib in rats by a simple high-performance liquid chromatography-tandem mass spectrometry method. Kim SB, Kim KT, Joo J, Seo KA, Hwang H, Kim SH, Song M, Lee S, Jahn A, Cho HJ, Kim DD, Yoon IS.Biomed Chromatogr. 2017 Feb;31(2). doi: 10.1002/bmc.3791. Epub 2016 Aug 8. PMID: 27432781 |
