产品名称

英文名称：Evacetrapib (LY2484595)

同义词

Evacetrapib、1186486-62-3、Evacetrapib (LY2484595)、LY2484595、LY-2484595、Evacetrapib [USAN]、LY 2484595、51XWV9K850、Evacetrapib (USAN)、(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

产品性质

CAS编号：1186486-62-3

分子式：C31H36F6N6O2

分子量：638.65

PubChem编号：49836058

英文别名：Evacetrapib|1186486-62-3|Evacetrapib (LY2484595)|LY2484595|LY-2484595|Evacetrapib [USAN]|LY 2484595|51XWV9K850|Evacetrapib (USAN)|(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

规格或纯度：≥98%

英文名称：Evacetrapib (LY2484595)

生化机理：Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. Evacetrapib (LY2484595) (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells. Evacetrapib (LY2484595) (30 mg/kg, orally) results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. Evacetrapib (LY2484595) (30 mg/kg) results in 129.7% increase in HDL-C 8 hours after oral administration. The ED50 values of CETP inhibitory activity 8 hours post oral dosing for Evacetrapib (LY2484595) in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. Evacetrapib (LY2484595) (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：卖完停产，不再备货

产品介绍：Evacetrapib (LY2484595)是高活性CETP选择性抑制剂，IC50为5.5 nM，能在不增加醛固酮和血压的情况下提高高密度脂蛋白胆固醇。Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure.

ALogP：7.7

IUPAC Name：4-[[(5S)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid

INCHI：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

InChi Key：IHIUGIVXARLYHP-UXNJHFGPSA-N

Canonical SMILES：CC1=CC(=C2C(=C1)C(CCCN2CC3CCC(CC3)C(=O)O)N(CC4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C5=NN(N=N5)C)C

Isomeric SMILES：CC1=CC(=C2C(=C1)[C@H](CCCN2CC3CCC(CC3)C(=O)O)N(CC4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C5=NN(N=N5)C)C

PubChem CID：49836058

Wikipedia：Evacetrapib

ChEMBL Ligand：CHEMBL2017179

CAS Registry No.：1186486-62-3

溶解性：DMSO 12.8 mg/mL Water <1 mg/mL Ethanol 12.8 mg/mL

象形图：

信号词：Warning

危险声明：H400 Very toxic to aquatic lifeH410 Very toxic to aquatic life with long lasting effectsH361 Suspected of damaging fertility or the unborn child

预防措施声明：P273,P280,P405,P501,P391,P203,P318

产品包装