Evacetrapib (LY2484595)

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

For research use only.

Catalog No.S2925

Evacetrapib (LY2484595) Chemical Structure

CAS No. 1186486-62-3

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.

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

Animal Research:^[1]	- Collapse Animal Models: Human ApoAI and CETP double transgenic mice Dosages: 30 mg/kg Administration: Orally (Only for Reference)

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

* 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 Information Download Evacetrapib (LY2484595) SDF

Molecular Weight	638.65
Formula	C₃₁H₃₆F₆N₆O₂
CAS No.	1186486-62-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
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)

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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.

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.

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Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
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Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

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

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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CETP Signaling Pathway Map

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