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Evacetrapib
产品别名
1186486-62-3
Evacetrapib
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
LY-2484595
LY 2484595
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
LY2484595
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C31H36F6N6O2 |
| Molecular weight | 638.65 |
| MDL number | MFCD23105886 |
| Biochem/physiol Actions【生化/生理作用】 | 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). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥95% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
| 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 |
