For research use only.
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.
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|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.|
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. 
|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. |
|In vitro||DMSO||12.8 mg/mL (20.04 mM)|
|Ethanol||12.8 mg/mL (20.04 mM)|
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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|
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