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Evacetrapib (LY2484595) CETP inhibitor

Name: Evacetrapib (LY2484595)
Brand: Selleck Chemicals
SKU: S2925
Availability: InStock
Rating: 5 (1 reviews)

Cat.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.

Chemical Structure

Molecular Weight: 638.65

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S292501 DMSO]12.8 mg/mL]false]Ethanol]12.8 mg/mL]false]Water]Insoluble]false Purity: 99.83%

99.83

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	Anacetrapib (MK-0859) Dalcetrapib (JTT-705)

Chemical Information, Storage & Stability

Molecular Weight	638.65	Formula	C₃₁H₃₆F₆N₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1186486-62-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

In vitro
Batch:

DMSO : 12.8 mg/mL ( (20.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12.8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	15% Captisol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (15.66mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 15% Captisol clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	CETP ^[1] 5.5 nM
In vitro	Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. This compound (< 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. This compound (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 this chemical in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. It (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats. ^[1]
References	https://pubmed.ncbi.nlm.nih.gov/21957197/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02497391	Completed	Healthy	Eli Lilly and Company	July 2015	Phase 1
NCT02365558	Completed	Healthy	Eli Lilly and Company	January 2015	Phase 1
NCT02271425	Completed	Healthy Volunteers	Eli Lilly and Company	October 2014	Phase 1
NCT02226653	Completed	Healthy Volunteers	Eli Lilly and Company	September 2014	Phase 1
NCT02156492	Completed	Healthy Volunteers	Eli Lilly and Company	June 2014	Phase 1
NCT02168803	Completed	Dyslipidemia	Eli Lilly and Company	May 2014	Phase 1

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