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Anacetrapib (MK-0859)

Catalog No.S2748

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5mg	USD 270	In stock
10mg	USD 370	In stock
50mg	USD 1070	In stock
200mg	USD 2470	In stock

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Technical Data

Molecular Weight (MW)	637.51
Formula	C₃₀H₂₅F₁₀NO₃
CAS No.	875446-37-0
Synonyms	N/A

Solubility (25°C)	DMSO 127 mg/mL
	Water <1 mg/mL
	Ethanol 127 mg/mL
Storage	2 years -20℃Powder
	2 weeks4℃in DMSO
	2 months-80℃in DMSO

Chemical Name	2-Oxazolidinone, 5-[3,5-bis(trifluoromethyl)phenyl]-3-[[4'-fluoro-2'-methoxy-5'-(1-methylethyl)-4-(trifluoromethyl)[1,1'-biphenyl]-2-yl]methyl]-4-methyl-, (4S,5R)-

Biological Activity

Description	Anacetrapib (MK0859) is a potent and selective rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, respectively
Targets	rhCETP	Mutant CETP (C13S)
IC50	7.9 nM	11.8 nM ^[1]
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]
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]
Clinical Trials	Anacetrapib is in a phase III study among people with established vascular disease.
Features

Protocol (Only for Reference)

Kinase Assay: ^[2]

Radioactive assays	The ability of Anacetrapib to block CETP-mediated CE and TG transfer is measured by radioactive CETP transfer assay with 2% human serum. The procedure is similar to the 95% human serum transfer assay, except that purified human HDL (128 μg/mL) and [³H] cholesteryl oleate or [³H] triolein-labeled LDL are used as acceptor and donor particles, respectively. The [³H] cholesteryl oleate or [³H] triolein from exogenous LDL to HDL is transferred by purified recombinant CETP (30 nM) in standard CETP Buffer (50 mM Tris pH 7.4, 100 nM NaCl, and 1 mM EDTA) with 2% human serum. The transfer reaction is terminated by precipitation of LDL with one volume of ice cold human serum and 2 volumes of 20% W/V PEG 8000. The samples are centrifuged and an aliquot of the HDL-containing supernatant is counted by liquid scintillation. Counts present in the supernatant for controls (without CETP addition) are subtracted from those reactivated with CETP to correct for non-specific transfer.

Radioactive assays

The ability of Anacetrapib to block CETP-mediated CE and TG transfer is measured by radioactive CETP transfer assay with 2% human serum. The procedure is similar to the 95% human serum transfer assay, except that purified human HDL (128 μg/mL) and [³H] cholesteryl oleate or [³H] triolein-labeled LDL are used as acceptor and donor particles, respectively. The [³H] cholesteryl oleate or [³H] triolein from exogenous LDL to HDL is transferred by purified recombinant CETP (30 nM) in standard CETP Buffer (50 mM Tris pH 7.4, 100 nM NaCl, and 1 mM EDTA) with 2% human serum. The transfer reaction is terminated by precipitation of LDL with one volume of ice cold human serum and 2 volumes of 20% W/V PEG 8000. The samples are centrifuged and an aliquot of the HDL-containing supernatant is counted by liquid scintillation. Counts present in the supernatant for controls (without CETP addition) are subtracted from those reactivated with CETP to correct for non-specific transfer.

Animal Study: ^[3]

Animal Models	Adult male Sprague-Dawley rats weighing 280 to 330 g
Formulation	In polyethylene glycol 300-water (7:3, v/v)
Dosages	2.5 mL/kg (2.5, 25, 50, 250 mg/mL)
Administration	Oral gavage

References

[1] Niesor EJ, et al. J Lipid Res. 2010, 51(12), 3443-3454.

[2] Ranalletta M, et al. J Lipid Res. 2010, 51(9), 2739-2752.

[3] Tan EY, et al. Drug Metab Dispos. 2010, 38(3), 459-473.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE

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