[CAS NO. 875446-37-0] Anacetrapib (MK-0859)

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Catalog:	SLK-S2748
Brand:	Selleck
CAS:	875446-37-0

Overview

MDL	MFCD16294903
Molecular Weight	637.51
Molecular Formula	C30H25F10NO3
SMILES	C(C1=C(C=CC(C(F)(F)F)=C1)C2=C(OC)C=C(F)C(C(C)C)=C2)N3[C@@H](C)[C@](OC3=O)(C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

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Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.5686 mL	7.8430 mL	15.6860 mL
5 mM	0.3137 mL	1.5686 mL	3.1372 mL
10 mM	0.1569 mL	0.7843 mL	1.5686 mL
50 mM	0.0314 mL	0.1569 mL	0.3137 mL

Description

Anacetrapib (MK0859) is a potent, selective, reversible and inhibitor with of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.

Targets

rhCETP ^[1]	Mutant CETP (C13S) ^[1]
7.9 nM	11.8 nM

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 [C]-dalcetrapibthiol bound to rhCETP. Anacetrapib decreases pre-β-HDL formation by more than 46%. Anacetrapib potently blocks CE and TG transfer in 95% human serum.

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. After oral administration of [C]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.

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.

Synonyms

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)-

(4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-[[4′-fluoro-2′-methoxy-5′-(1-methylethyl)-4-(trifluoromethyl)[1,1′-biphenyl]-2-yl]methyl]-4-methyl-2-oxazolidinone

(4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-[[4′-fluoro-5′-isopropyl-2′-methoxy-4-(trifluoromethyl)biphenyl-2-yl]methyl]-4-methyl-1,3-oxazolidin-2-one

Anacetrapib

MK 0859

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