Evacetrapib (LY2484595)

Catalog No.S2925

For research use only.

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

CAS No. 1186486-62-3

Purity & Quality Control

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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

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 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]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Human ApoAI and CETP double transgenic mice
  • Dosages: 30 mg/kg
  • Administration: Orally

Solubility (25°C)

In vitro

DMSO 12.8 mg/mL
(20.04 mM)
Ethanol 12.8 mg/mL
(20.04 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 638.65
Formula

C31H36F6N6O2

CAS No. 1186486-62-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02497391 Completed Drug: Evacetrapib Healthy Eli Lilly and Company July 2015 Phase 1
NCT02365558 Completed Drug: Evacetrapib|Drug: Omeprazole Healthy Eli Lilly and Company January 2015 Phase 1
NCT02271425 Completed Drug: Evacetrapib Tablet|Drug: Evacetrapib Intravenous Healthy Volunteers Eli Lilly and Company October 2014 Phase 1
NCT02226653 Completed Drug: Evacetrapib Healthy Volunteers Eli Lilly and Company September 2014 Phase 1
NCT02156492 Completed Drug: Evacetrapib|Drug: Simvastatin|Drug: Atorvastatin Healthy Volunteers Eli Lilly and Company June 2014 Phase 1
NCT02168803 Completed Drug: Evacetrapib Dyslipidemia Eli Lilly and Company May 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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