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Apabetalone

Name: Apabetalone
Brand: TargetMol
SKU: T2480
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2480Cas No. 1044870-39-4

Alias RVX-208, RVX000222

Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.

Apabetalone

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Purity: 99.89%

Catalog No. T2480Alias RVX-208, RVX000222Cas No. 1044870-39-4

Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$39	In Stock	In Stock
25 mg	$72	In Stock	In Stock
50 mg	$119	In Stock	In Stock
100 mg	$173	In Stock	In Stock
500 mg	$429	-	In Stock
1 mL x 10 mM (in DMSO)	$43	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.89%

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.
Targets&IC50	BD2:0.51 μM
In vitro	In AGMs, RVX-208 significantly increases serum apoA-I and HDL-C levels and enhances cholesterol efflux through various pathways.
In vivo	In vitro studies have demonstrated that RVX-208 activates the expression of the apolipoprotein AI gene, leading to an increase in apoA-I and HDL-C levels. Additionally, RVX-208 inhibits BET bromodomain proteins, exhibiting a preferential binding to the second bromodomain of BET proteins.
Cell Research	RVX-208 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 μM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 μg/mL for 3 hours[2].
Synonyms	RVX-208, RVX000222

Chemical Properties

Molecular Weight	370.4
Formula	C₂₀H₂₂N₂O₅
Cas No.	1044870-39-4
Smiles	COc1cc(OC)c2c(c1)[nH]c(nc2=O)-c1cc(C)c(OCCO)c(C)c1
Relative Density.	1.28 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 27.32 mg/mL (73.76 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.4 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6998 mL	13.4989 mL	26.9978 mL	134.9892 mL
5 mM	0.5400 mL	2.6998 mL	5.3996 mL	26.9978 mL
10 mM	0.2700 mL	1.3499 mL	2.6998 mL	13.4989 mL
20 mM	0.1350 mL	0.6749 mL	1.3499 mL	6.7495 mL
50 mM	0.0540 mL	0.2700 mL	0.5400 mL	2.6998 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc