Evacetrapib (LY2484595)

Catalog No.S2925

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.

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Evacetrapib (LY2484595) Chemical Structure

Evacetrapib (LY2484595) Chemical Structure
Molecular Weight: 638.65

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Binding assay The medium contains the secreted recombinant CETP protein and the amount (19 ng/μL) is quantified by an ELISA kit. The medium is then aliquoted in 0.2% BSA and stored at -80℃. The stock CETP protein is diluted 150-fold in CETP buffer (10 mM Tris, 150 mM NaCl, and 2 mM EDTA) before use. The assay is set up in a 96-well plate. Each well receives 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of compound stock. After a 30 min incubation at 37 ℃, 5 μL of substrate stock, 0.16 μL of VLDL stock (2.5 mg/mL) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 hours. The fluorescent signal is measured in a fluorescent plate reader with 544 nm excitation and 595 nm emission upon the transfer of fluorescent cholesterol ester analogs to apoB-containing lipoproteins. IC50 values (concentration of compound causing a 50% inhibition of CETP activity) are determined by nonlinear regression.

Animal Study: [1]

Animal Models Human ApoAI and CETP double transgenic mice
Formulation 10% acacia
Dosages 30 mg/kg
Administration Orally
Solubility 15% Captisol, , 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

[1] Cao G, et al. J Lipid Res, 2011, 52(12), 2169-2176.

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01825889 Completed Cardiovascular Disease Eli Lilly and Company 2013-04 Phase 1
NCT01903434 Completed Healthy Volunteers Eli Lilly and Company 2013-07 Phase 1
NCT01908582 Completed Healthy Volunteers Eli Lilly and Company 2013-07 Phase 1
NCT01897493 Completed Healthy Volunteers Eli Lilly and Company 2013-07 Phase 1
NCT01958489 Completed Healthy Volunteers Eli Lilly and Company 2013-10 Phase 1

Chemical Information

Molecular Weight (MW) 638.65
Formula

C31H36F6N6O2

CAS No. 1186486-62-3
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 12.8 mg/mL (20 mM)
Water <1 mg/mL (<1 mM)
Ethanol 12.8 mg/mL (20 mM)
In vivo 15% Captisol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 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-

Research Area

Tech Support & FAQs

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.

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