Evacetrapib (LY2484595) - Moligand™, 10mM in DMSO , Cholesteryl ester transfer protein inhibitor, CAS No.1186486-62-3, Cholesteryl ester transfer protein inhibitor

CAS: 1186486-62-3 Cat. No.: E408279 Molecular Weight: 638.65 EC Number: 800-517-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Cyclohexanecarboxylic acid, 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]-, trans-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Evacetrapib (LY2484595) 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. Phase 3.
In vitro

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.

In vivo

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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

Cyclohexanecarboxylic acid, 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]-, trans-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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. Phase 3.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Cholesteryl ester transfer protein inhibitor

Product Properties

• ALogP: 7.7

Names and Identifiers

• 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
• Molecular Weight: 638.65
• Reaxy-Rn: 38962088
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=38962088&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro