In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
Anacetrapib (MK-0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM. It increases HDL-C and decreases LDL-C, and does not increase aldosterone or blood pressure. This compound is in Phase 3.
Targets
rhCETP
Mutant CETP (C13S)
7.9 nM
11.8 nM
In vitro
Anacetrapib (MK-0859) is not only able to increase HDL-cholesterol, but also further decreases LDL-cholesterol when taken in combination with a statin. It dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2. This compound doesn't affect the amount of [14C]-dalcetrapibthiol bound to rhCETP. It decreases pre-β-HDL formation by more than 46%. Anacetrapib potently blocks CE and TG transfer in 95% human serum.
In Vivo
In a dyslipidaemic hamster model, 60 mg/kg/day Anacetrapib (MK-0859) 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. This compound also promotes reverse cholesterol transport from macrophages, and leads to a 30% increase in faecal cholesterol content. HDL from it-treated hamsters reveals an increase in SR-B1- and ABCG1-mediated efflux compared with controls. After oral administration of [14C]Anacetrapib at 10 mg/kg, ~80 and 90% of the radioactive dose is recovered over 48 hours postdose from rats and monkeys, respectively. The majority of the administered radioactive dose is excreted unchanged in faeces in both species.
Adult male Sprague-Dawley rats weighing 280 to 330 g
Dosages
2.5 mL/kg (2.5, 25, 50, 250 mg/mL)
Administration
Oral gavage
References
https://pubmed.ncbi.nlm.nih.gov/20861162/
https://pubmed.ncbi.nlm.nih.gov/20458119/
https://pubmed.ncbi.nlm.nih.gov/20016052/
Sellecks Anacetrapib (MK-0859) Has Been Cited by 3 Publications
Inhibition of Cholesteryl Ester Transfer Protein Preserves High-Density Lipoprotein Cholesterol and Improves Survival in Sepsis
[ Circulation, 2021, 143(9):921-934]
CETP inhibitors downregulate hepatic LDL receptor and PCSK9 expression in vitro and in vivo through a SREBP2 dependent mechanism.
[ Atherosclerosis, 2014, 235(2):449-62]
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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