Evacetrapib (LY2484595)

Catalog No.S2925

Evacetrapib (LY2484595) Chemical Structure

Molecular Weight(MW): 638.65

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.

Size Price Stock Quantity  
In DMSO USD 540 In stock
USD 210 In stock
USD 270 In stock
USD 970 In stock
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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]
+ Expand
  • Animal Models: Human ApoAI and CETP double transgenic mice
  • Formulation: 10% acacia
  • Dosages: 30 mg/kg
  • Administration: Orally
    (Only for Reference)

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 individually and in order:
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.

Chemical Information

Molecular Weight 638.65
Formula

C31H36F6N6O2

CAS No. 1186486-62-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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
NCT02260648 Terminated Hypercholesterolemia Eli Lilly and Company January 2015 Phase 3
NCT02260635 Terminated Hypercholesterolemia Eli Lilly and Company November 2014 Phase 3
NCT02271425 Completed Healthy Volunteers Eli Lilly and Company October 2014 Phase 1
NCT02227784 Terminated Hyperlipidemia Eli Lilly and Company October 2014 Phase 3

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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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CETP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID