[CAS NO. 1044870-39-4] Apabetalone (RVX-208)

Name: Apabetalone (RVX-208)
Brand: Arctom Scientific
SKU: SLK-S7295

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PRODUCTS SPECIFICATIONS [1044870-39-4]

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Catalog

SLK-S7295

Brand

Selleck

CAS

1044870-39-4

DESCRIPTION [1044870-39-4]

Overview

MDL	MFCD18633270
Molecular Weight	370.4
Molecular Formula	C20H22N2O5
SMILES	O(C)C1=C2C(NC(=NC2=O)C3=CC(C)=C(OCCO)C(C)=C3)=CC(OC)=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6998 mL	13.4989 mL	26.9978 mL
5 mM	0.5400 mL	2.6998 mL	5.3996 mL
10 mM	0.2700 mL	1.3499 mL	2.6998 mL
50 mM	0.0540 mL	0.2700 mL	0.5400 mL

Description

Apabetalone (RVX-208, RVX-000222) is a potent inhibitor with of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.

Features

First-in-class BD2-selective inhibitor of BET bromodomain and has been tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis.

Targets

BD2 ^[1]
(Cell-free assay)

0.51 μM

In vitro

As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro.

In vivo

RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways.

References

[1] Picaud S, et al. Proc Natl Acad Sci U S A. 2013, 110(49), 19754-19759.
[2] McNeill E. Curr Opin Investig Drugs. 2010, 11(3), 357-364.
[3] Bailey D, et al. J Am Coll Cardiol. 2010, 55(23), 2580-2589.

Synonyms

4(3H)-Quinazolinone, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-

2-[4-(2-Hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone

2-[4-(2-Hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-3H-quinazolin-4-one

2-[4-(2-Hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one

RVX 208

RVX 000222

Apabetalone

2-[4-(2-Hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1H-quinazolin-4-one