Anacetrapib (MK-0859)

Name: Anacetrapib (MK-0859)
Brand: Selleck Chemicals
SKU: S2748
Rating: 5 (3 reviews)

For research use only.

Catalog No.S2748

3 publications

Anacetrapib (MK-0859) Chemical Structure

CAS No. 875446-37-0

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.

Selleck's Anacetrapib (MK-0859) has been cited by 3 publications

Circulation, 2021, 143(9):921-934

PubMed: 33228395 ( click the link to review the publication )

J Phys Chem B, 2016, 120(33):8254-63

PubMed: 27111423 ( click the link to review the publication )

Atherosclerosis, 2014, 235(2):449-62

PubMed: 24950000 ( click the link to review the publication )

Purity & Quality Control

Choose Selective CETP Inhibitors

Biological Activity

Description

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 [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]

Protocol

Animal Research: ^[3]	- Collapse Animal Models: 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 (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	127 mg/mL (199.21 mM)
	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 Download Anacetrapib (MK-0859) SDF

Molecular Weight	637.51
Formula	C₃₀H₂₅F₁₀NO₃
CAS No.	875446-37-0
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1C(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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
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Molecular Weight Calculator

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01122667	Completed	Drug: anacetrapib	Dyslipidemia	Merck Sharp & Dohme Corp.	June 2010	Phase 1
NCT01114490	Completed	Drug: anacetrapib	Dyslipidemia	Merck Sharp & Dohme Corp.	May 2010	Phase 1
NCT00325455	Terminated	Drug: MK0859	Hypercholesterolemia\|Mixed Hyperlipemia	Merck Sharp & Dohme Corp.	June 2006	Phase 2

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.

Handling Instructions

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CETP Signaling Pathway Map

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Anacetrapib (MK-0859)