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Merck
CN

SML3085

Evacetrapib

≥95% (HPLC)

Synonym(s):

LY 2484595, LY-2484595, LY2484595, trans-4-({(5S)-5-[{[3,5-bis(Trifluoromethyl)phenyl]methyl}(2-methyl-2H-tetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1H-benzazepin-1-yl}methyl)cyclohexanecarboxylic acid, trans-4-[[(5S)-5-[[[3,5-bis(Trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid

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About This Item

Empirical Formula (Hill Notation):
C31H36F6N6O2
CAS Number:
1186486-62-3
Molecular Weight:
638.65
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD23105886
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
100

Key Documents

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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 string

CC1=C2C([C@@H](N(CC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C4=NN(C)N=N4)CCCN2C[C@H]5CC[C@H](C(O)=O)CC5)=CC(C)=C1

InChI key

IHIUGIVXARLYHP-UXNJHFGPSA-N

assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Evacetrapib (LY2484595) is an orally active, potent and selective cholesteryl ester transfer protein (CETP) inhibitor (human recombinant CETP IC50 = 5.5 nM). Evacetrapib inhibits CETP activtiy in human plasma ex vivo (IC50 = 36 nM) and in human CETP/ApoAI transgenic mice in vivo (129.7% HDL-C increase 8 h post oral dosing at 30 mg/kg; 98.4%, 98.6%, 18.4% CETP inhibition, respectivley, post 4, 8 and 24 h p.o.). Evacetrapib does not cause the side-effects observed with torcetrapib in cultures (no aldosterone or cortisol synthesis induction in H295R cells) or in vivo (no increase of mean arterial pressure in diabetic fatty rats).
Orally active, potent and selective cholesteryl ester transfer protein (CETP) inhibitor in vitro and in vivo.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000134523
0000134524
0000130192

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