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.

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In DMSO USD 540 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 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

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
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
NCT02365558 Completed Healthy Eli Lilly and Company January 2015 Phase 1
NCT02260648 Terminated Hypercholesterolemia Eli Lilly and Company January 2015 Phase 3

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CETP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID