Anacetrapib (MK-0859)
Catalog No.S2748
Molecular Weight(MW): 637.51
Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.
Purity & Quality Control
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Biological Activity
| Description | Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3. | ||||
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| In vitro |
Anacetrapib is not only able to increase HDL-cholesterol, but also further decreases LDL-cholesterol when taken in combination with a statin. Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2. Anacetrapib doesn't affect the amount of [14C]-dalcetrapibthiol bound to rhCETP. Anacetrapib decreases pre-β-HDL formation by more than 46%. [1] Anacetrapib potently blocks CE and TG transfer in 95% human serum.[2] |
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| In vivo | In a dyslipidemic hamster model, 60 mg/kg/day Anacetrapib for 2 weeks results in a 94% reduction in CETP activity and 47% increase in HDL-cholesterol compared with control animals; non-HDL-cholesterol concentrations are not affected. In addition, Anacetrapib promotes reverse cholesterol transport from macrophages, and leads to a 30% increase in fecal cholesterol content. HDL from Anacetrapib-treated hamsters reveals an increase in SR-B1- and ABCG1-mediated efflux compared with controls. [2] After oral administration of [14C]Anacetrapib at 10 mg/kg, ∼80 and 90% of the radioactive dose is recovered over 48 hous postdose from rats and monkeys, respectively. The majority of the administered radioactive dose is excreted unchanged in feces in both species. [3] |
Protocol
| Animal Research: [3] |
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Solubility (25°C)
| In vitro | DMSO | 127 mg/mL (199.21 mM) |
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| Ethanol | 127 mg/mL (199.21 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing. |
10 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 | 637.51 |
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| Formula | C30H25F10NO3 |
| CAS No. | 875446-37-0 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01717300 | Completed | Hypercholesterolemia | Merck Sharp & Dohme Corp. | November 6 2012 | Phase 3 |
| NCT01524289 | Active not recruiting | Hyperlipoproteinemia Type II|Heterozygous Familial Hypercholesterolemia | Merck Sharp & Dohme Corp. | February 3 2012 | Phase 3 |
| NCT00685776 | Completed | Coronary Heart Disease (CHD)|CHD Risk-Equivalent Disease | Merck Sharp & Dohme Corp. | March 24 2008 | Phase 3 |
| NCT02931188 | Completed | Atherosclerotic Cardiovascular Disease|Vascular Disease | Cambridge University Hospitals NHS Foundation Trust|British Heart Foundation Cambridge Centre of Excellence | January 2017 | -- |
| NCT01841684 | Terminated | Hyperlipoproteinemia Type II|Homozygous Familial Hypercholesterolemia | Merck Sharp & Dohme Corp. | June 2013 | Phase 3 |
| NCT01860729 | Completed | Hypercholesterolemia | Merck Sharp & Dohme Corp. | May 2013 | Phase 3 |
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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