Anacetrapib (MK-0859)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
100mg	$850	Check With Us
250mg	$1400	Check With Us
500mg	$2100	Check With Us

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Cat #: V0911 CAS #: 875446-37-0 Purity ≥ 98%

Description: Anacetrapib (formerly also known as MK0859; MK-0859), a poly-fluorinated lipophilic compound, is a selective and reversible inhibitor of CETP (Cholesteryl ester transfer protein) and mutant CETP(C13S) with the potential to treat cardiovascular disease.

References: Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	637.51
Molecular Formula	C30H25F10NO3
CAS No.	875446-37-0
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 127 mg/mL (199.2 mM)r
	Water: <1 mg/mLr
	Ethanol: 127 mg/mL (199.2 mM)
Solubility In Vivo	30% PEG400+0.5% Tween80+5% propylene glycol: 10 mg/mL
SMILES Code	O=C1O[C@H](C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)[C@H](C)N1CC3=CC(C(F)(F)F)=CC=C3C4=CC(C(C)C)=C(F)C=C4OC
Synonyms	MK 0859; Anacetrapib; MK0859; MK-0859;

Protocol	In Vitro	Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2 (P<0.001 for concentrations equal to and higher than 0.1 µM). Excess Anacetrapib (25 µM) decreases the amount of [14C]Torcetrapib (0.25 µM) binds to immobilized rhCETP by 82% and 60%, respectively. Anacetrapib decreases pre-β-HDL formation by more than 46% (P<0.001) at all concentrations tested (0.1, 1, 3, and 10 µM).
Protocol	In Vivo	Hamsters are given Anacetrapib for 7 days before injection of [3H]cholesterol-labeled macrophages (day 0). Treatment with Anacetrapib leads to significant increases in HDL-C levels at day 0. At day 3, [3H]cholesterol radioactivity in the HDL fraction is significantly increased from control values for Anacetrapib.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.5686 mL	7.8430 mL	15.6860 mL	31.3721 mL
5mM	0.3137 mL	1.5686 mL	3.1372 mL	6.2744 mL
10mM	0.1569 mL	0.7843 mL	1.5686 mL	3.1372 mL
20mM	0.0784 mL	0.3922 mL	0.7843 mL	1.5686 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.