Anacetrapib (MK-0859) - Moligand™, 10mM in DMSO , Cholesteryl ester transfer protein inhibitor, CAS No.875446-37-0, Cholesteryl ester transfer protein inhibitor

CAS: 875446-37-0 Cat. No.: A407745 Molecular Weight: 637.51 EC Number: 810-468-5

GRADE & PURITY Moligand™, 10mM in DMSO

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)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Anacetrapib (MK-0859) 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.
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%. 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 [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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

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)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Cholesteryl ester transfer protein inhibitor

Product Properties

• ALogP: 8.8

Names and Identifiers

• Isomeric SMILES: C[C@H]1[C@H](OC(=O)N1CC2=C(C=CC(=C2)C(F)(F)F)C3=CC(=C(C=C3OC)F)C(C)C)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F
• Molecular Weight: 637.51
• Reaxy-Rn: 43874221
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=43874221&ln=

Associated Targets(Human)

CETP Tchem Cholesteryl ester transfer protein (12 Activities)

Discover Target: CETP

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro