SML3085

Evacetrapib

≥95% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₃₁H₃₆F₆N₆O₂
• CAS-Nummer: 1186486-62-3
• Molekulargewicht: 638.65
• UNSPSC Code: 51111800
• NACRES: NA.77
• MDL number: MFCD23105886
• Assay: ≥95% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• 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: 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

Beschreibung

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.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable