Home Metabolism CETP inhibitor Evacetrapib (LY2484595) For research use only.

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.

Evacetrapib (LY2484595) Chemical Structure

Evacetrapib (LY2484595) Chemical Structure

CAS No. 1186486-62-3

Purity & Quality Control

Batch: S292501 DMSO]12.8 mg/mL]false]Ethanol]12.8 mg/mL]false]Water]Insoluble]false Purity: 99.83%
99.83

Evacetrapib (LY2484595) Related Products

Signaling Pathway

CETP Signaling Pathways

CETP Signaling Pathway

Biological Activity

Description 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.
Targets
CETP [1]
5.5 nM
In vitro
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. [1]
In Vivo
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. [1]
Animal Research Animal Models Human ApoAI and CETP double transgenic mice
Dosages 30 mg/kg
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02497391 Completed
Healthy
Eli Lilly and Company
 July 2015 Phase 1
NCT02365558 Completed
Healthy
Eli Lilly and Company
 January 2015 Phase 1
NCT02271425 Completed
Healthy Volunteers
Eli Lilly and Company
 October 2014 Phase 1
NCT02226653 Completed
Healthy Volunteers
Eli Lilly and Company
 September 2014 Phase 1
NCT02156492 Completed
Healthy Volunteers
Eli Lilly and Company
 June 2014 Phase 1
NCT02168803 Completed
Dyslipidemia
Eli Lilly and Company
 May 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 638.65 Formula

C31H36F6N6O2
CAS No. 1186486-62-3 SDF Download Evacetrapib (LY2484595) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 12.8 mg/mL ( (20.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12.8 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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