Evacetrapib (LY2484595)

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

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Size	Price	Stock
250mg	$1250	Check With Us
500mg	$1850	Check With Us
1g	$2775	Check With Us

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Cat #: V0913 CAS #: 1186486-62-3 Purity ≥ 98%

Description: Evacetrapib (also known as LY-2484595; LY2484595), a benzazepine compound, is a potent and selective inhibitor of CETP (Cholesteryl ester transfer protein) with the potential to lower cholesterol levels and to prevent cardiovascular diseases.

References: Cao G, et al. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J Lipid Res. 2011 Dec;52(12):2169-76.

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

Molecular Weight (MW)	638.65
Molecular Formula	C31H36F6N6O2
CAS No.	1186486-62-3
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 12.8 mg/mL (20.0 mM)r
	Water: <1 mg/mLr
	Ethanol: 12.8 mg/mL (20.0 mM)
Solubility In Vivo	15% Captisol: 30 mg/mL
SMILES Code	O=C([C@H]1CC[C@H](CN2C3=C(C)C=C(C)C=C3[C@@H](N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C5=NN(C)N=N5)CCC2)CC1)O
Synonyms	Evacetrapib; LY 2484595; LY2484595; LY-2484595

Protocol	In Vitro	Evacetrapib is a novel benzazepine-based CETP inhibitor. In the buffer CETP assay, the absolute potency of the compound is 5.5 nM. In the human plasma CETP assay, the CETP concentration is about 2 μg/mL (25 nM) and the 36 nM IC50 value again indicates that Evacetrapib is a potent CETP inhibitor against either the recombinant protein or CETP from human plasma. Evacetrapib is apparently much more potent than Dalcetrapib.
Protocol	In Vivo	In double transgenic mice expressing human CETP and apoAI, Evacetrapib exhibits an ex vivo CETP inhibition ED50 of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. Importantly, no blood pressure elevation is observed in rats dosed with Evacetrapib at high exposure multiples compared with the positive control, torcetrapib. Evacetrapib administered orally at 30 mg/kg results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4, 8 and 24 h post dose respectively. Evacetrapib dosed orally at 30 mg/kg resulted in 129.7% increase in HDL-C 8 h after oral administration.

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	1.5658 mL	7.8290 mL	15.6580 mL	31.3161 mL
5mM	0.3132 mL	1.5658 mL	3.1316 mL	6.2632 mL
10mM	0.1566 mL	0.7829 mL	1.5658 mL	3.1316 mL
20mM	0.0783 mL	0.3915 mL	0.7829 mL	1.5658 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.