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Evacetrapib (LY2484595)

Name: Evacetrapib (LY2484595)
Brand: Selleck Chemicals
SKU: S2925
Rating: 5 (0 reviews)

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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CETP Signaling Pathway Map

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

References

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

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
Storage	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

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In vivo Formulation Calculator (Clear solution)

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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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Molarity Calculator

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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)

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