WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510227
Description: Evacetrapib, also known as LY2484595, is a CETP inhibitor currently under development by Eli Lilly & Company. LY2484595 inhibits cholesterylester transfer protein, which transfers and thereby increases high-density lipoprotein and lowers low-density lipoprotein. It is thought that modifying lipoprotein levels modifies the risk of cardiovascular disease. The first CETP inhibitor, torcetrapib, was unsuccessful because it increased levels of the hormone aldosterone and increased blood pressure, which led to excess cardiac events when it was studied. Evacetrapib does not have the same effect. When studied in a small clinical trial in people with elevated LDL and low HDL, significant improvements were noted in their lipid profile. (Source: http://en.wikipedia.org/wiki/Evacetrapib).
MedKoo Cat#: 510227
Chemical Formula: C31H36F6N6O2
Exact Mass: 638.28039
Molecular Weight: 638.65
Elemental Analysis: C, 58.30; H, 5.68; F, 17.85; N, 13.16; O, 5.01
Synonym: LY2484595; LY 2484595; LY-2484595; Evacetrapib.
IUPAC/Chemical Name: (1S,4r)-4-(((S)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2H-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
InChi Key: IHIUGIVXARLYHP-YBXDKENTSA-N
InChi Code: InChI=1S/C31H36F6N6O2/c1-18-11-19(2)27-25(12-18)26(5-4-10-42(27)16-20-6-8-22(9-7-20)28(44)45)43(29-38-40-41(3)39-29)17-21-13-23(30(32,33)34)15-24(14-21)31(35,36)37/h11-15,20,22,26H,4-10,16-17H2,1-3H3,(H,44,45)/t20-,22-,26-/m0/s1
SMILES Code: O=C([C@H]1CC[C@H](CN2C3=C(C)C=C(C)C=C3[C@@H](N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C5=NN(C)N=N5)CCC2)CC1)O
Evacetrapib is one of two CETP inhibitors currently being evaluated (the other being anacetrapib). Two other CETP inhibitors (torcetrapib and dalcetrapib) were discontinued during trials due to increased deaths and little identifiable cardiovascular benefit (despite substantial increases in HDL). Some hypothesize that CETP inhibitors may still be useful in the treatment of dyslipidemia, though significant caution is warranted. (source: http://en.wikipedia.org/wiki/Evacetrapib).
1: Suico JG, Friedrich S, Krueger KA, Zhang W. Evacetrapib at a Supratherapeutic Steady State Concentration Does Not Prolong QT in a Thorough QT/QTc Study in Healthy Participants. J Cardiovasc Pharmacol Ther. 2013 Nov 22. [Epub ahead of print] PubMed PMID: 24271137.
2: Steen DL, Cannon CP. Atherosclerosis. Effects of evacetrapib administered as monotherapy or in combination with statins. Rev Cardiovasc Med. 2012;13(1):e48-51. PubMed PMID: 22754969.
3: Nicholls SJ. Evacetrapib. Curr Cardiol Rep. 2012 Jun;14(3):245-50. doi: 10.1007/s11886-012-0252-3. Review. PubMed PMID: 22362199.
4: Mearns BM. Pharmacotherapy: Beneficial effects of evacetrapib. Nat Rev Cardiol. 2011 Nov 29;9(1):6. doi: 10.1038/nrcardio.2011.193. PubMed PMID: 22124317.
5: Nicholls SJ, Brewer HB, Kastelein JJ, Krueger KA, Wang MD, Shao M, Hu B, McErlean E, Nissen SE. Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial. JAMA. 2011 Nov 16;306(19):2099-109. doi: 10.1001/jama.2011.1649. PubMed PMID: 22089718.
6: Cao G, Beyer TP, Zhang Y, Schmidt RJ, Chen YQ, Cockerham SL, Zimmerman KM, Karathanasis SK, Cannady EA, Fields T, Mantlo NB. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J Lipid Res. 2011 Dec;52(12):2169-76. doi: 10.1194/jlr.M018069. Epub 2011 Sep 25. PubMed PMID: 21957197; PubMed Central PMCID: PMC3220285.