Evacetrapib (Synonyms: LY2484595)

Name: Evacetrapib
Brand: MedChemExpress
SKU: HY-13327
Rating: 5.0 (3 reviews)

Cat. No.: HY-13327 Purity: 98.89%: FAQs
Data Sheet SDS COA Handling Instructions

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Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC₅₀ 5.5 nM) and CETP activity in human plasma (IC₅₀ 36 nM) in vitro.

For research use only. We do not sell to patients.

Evacetrapib Chemical Structure

CAS No. : 1186486-62-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 91	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 91	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 65	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 245	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE Evacetrapib

: Evacetrapib purchased from MedChemExpress. Usage Cited in: Atherosclerosis. 2014 Aug;235(2):449-62. [Abstract]; Downregulation of SREBP2-M by EVA and TOR reduced LDLR and PCSK9 expression. HepG2 cells are treated with EVA at indicated concentrations for 24 h. Total cell lysates (30 µg) are analyzed for the protein abundance of LDLR and β-actin. Nuclear and cytoplasmic extracts are isolated from each sample. Nuclear extracts of 30 µg protein per sample are used to detect SREBP2-M. The membrane is reprobed with anti-HDAC1. Cytoplasmic extracts of 30 µg protein per sample are used to detect SREBP2-P. The mem

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Protocol
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Description

Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC₅₀ 5.5 nM) and CETP activity in human plasma (IC₅₀ 36 nM) in vitro.

IC₅₀ & Target

IC50: 5.5 nM (CETP)^[1]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

638.65

Formula

C₃₁H₃₆F₆N₆O₂

CAS No.

1186486-62-3

Appearance

Solid

Color

White to light yellow

SMILES

O=C([C@H]1CC[C@H](CN2CCC[C@H](N(CC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C4=NN(C)N=N4)C5=CC(C)=CC(C)=C52)CC1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (156.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5658 mL	7.8290 mL	15.6580 mL
5 mM	0.3132 mL	1.5658 mL	3.1316 mL
10 mM	0.1566 mL	0.7829 mL	1.5658 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.89%

Select Batch:

Data Sheet (280 KB) SDS (562 KB)

COA (255 KB) RP-HPLC (243 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

Kinase Assay ^[1]	Human CETP cDNA is amplified from a human liver cDNA library and the sequence is confirmed to be identical to the published sequence. The cDNA is subcloned into a pcDNA3.1 vector, under the control of CMV promoter. A stable line is established in CV1 cells in which the above-mentioned construct is used to express the recombinant human CETP. The medium contained the secreted recombinant CETP protein and the amount (19 ng/μL) is quantified by an ELISA kit. The medium is then aliquoted in 0.2% BSA and stored at -80°C. The stock CETP protein is diluted 150-fold in CETP buffer (10 mM Tris, 150 mM NaCl, and 2 mM EDTA) before use. The assay is set up in a 96-well plate. Each well received 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of compound stock. After a 30 min incubation at 37°C, 5 μL of substrate stock (the same stock used in the human plasma CETP assay), 0.16 μL of VLDL stock (2.5 mg/mL, Intracel) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 h. Signal is read for the human plasma CETP assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] The blood pressure study is carried out using telemetered, male, obese Zucker Diabetic rats (ZDF fa/fa rats, 8 weeks of age on arrival; n=4). All rats underwent surgical implantation of a telemetry transmitter for continuous monitoring of hemodynamic parameters throughout the study. The rats are acclimated on Purina 5008 chow and house water ad libitum until 11 weeks of age. Mean daily blood pressure for the 24-h period immediately prior to administration of compound is taken as the baseline blood pressure. On the day of an experiment, a single 160 mg/kg dose (in 10% acacia) of Evacetrapib as the lysine salt is administered by oral gavage, and the drug effect is taken as the average daily mean arterial pressure (MAP) during the 24 h period following the dose. Data are expressed as the change in MAP from baseline. Following the last day of blood pressure monitoring, samples are collected from the orbital sinus at 1, 2, 4, 8, and 24 h post dose into tubes containing EDTA and processed into plasma. Plasma concentrations of Evacetrapib are measured using liquid chromatography tandem mass spectrometry. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5658 mL	7.8290 mL	15.6580 mL	39.1451 mL
	5 mM	0.3132 mL	1.5658 mL	3.1316 mL	7.8290 mL
	10 mM	0.1566 mL	0.7829 mL	1.5658 mL	3.9145 mL
	15 mM	0.1044 mL	0.5219 mL	1.0439 mL	2.6097 mL
	20 mM	0.0783 mL	0.3915 mL	0.7829 mL	1.9573 mL
	25 mM	0.0626 mL	0.3132 mL	0.6263 mL	1.5658 mL
	30 mM	0.0522 mL	0.2610 mL	0.5219 mL	1.3048 mL
	40 mM	0.0391 mL	0.1957 mL	0.3915 mL	0.9786 mL
	50 mM	0.0313 mL	0.1566 mL	0.3132 mL	0.7829 mL
	60 mM	0.0261 mL	0.1305 mL	0.2610 mL	0.6524 mL
	80 mM	0.0196 mL	0.0979 mL	0.1957 mL	0.4893 mL
	100 mM	0.0157 mL	0.0783 mL	0.1566 mL	0.3915 mL

Evacetrapib Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Evacetrapib1186486-62-3LY2484595LY 2484595LY-2484595CETPCholesteryl ester transfer proteinInhibitorinhibitorinhibit

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Evacetrapib (Synonyms: LY2484595)

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Evacetrapib Related Antibodies

2 Publications Citing Use of MCE Evacetrapib

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Complete Stock Solution Preparation Table

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