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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

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

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-09-13)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02227784 Not yet recruiting Hyperlipidemia Eli Lilly and Company October 2014 Phase 3
NCT02226653 Not yet recruiting Healthy Volunteers Eli Lilly and Company September 2014 Phase 1
NCT02161731 Recruiting Healthy Volunteers Eli Lilly and Company June 2014 Phase 1
NCT02156492 Recruiting Healthy Volunteers Eli Lilly and Company June 2014 Phase 1
NCT02168803 Recruiting Dyslipidemia Eli Lilly and Company May 2014 Phase 1

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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-

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