SML3085

Evacetrapib

≥95% (HPLC)

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₃₁H₃₆F₆N₆O₂
• Número de CAS: 1186486-62-3
• Peso molecular: 638.65
• Número MDL: MFCD23105886
• Código UNSPSC: 51111800
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: powder
• color: white to beige
• solubilidad: DMSO: 2 mg/mL, clear
• temp. de almacenamiento: −20°C
• cadena SMILES: 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: 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
• Clave InChI: IHIUGIVXARLYHP-UXNJHFGPSA-N

Descripción

Acciones bioquímicas o fisiológicas

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.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable