Evacetrapib (LY2484595)
Catalog No.S2925
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.
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. | ||
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| 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] |
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| 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] |
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Solubility (25°C)
| In vitro | DMSO | 12.8 mg/mL (20.04 mM) |
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| 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 |
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| Formula | C31H36F6N6O2 |
| CAS No. | 1186486-62-3 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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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 |
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.
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