GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

RVX-000222 | 4(3H)​-​Quinazolinone, 2-​[4-​(2-​hydroxyethoxy)​-​3,​5-​dimethylphenyl]​-​5,​7-​dimethoxy-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Apabetalone (RVX-208) Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.
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.
Cell Data

cell lines：CV-1 cells

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

RVX-000222 | 4(3H)​-​Quinazolinone, 2-​[4-​(2-​hydroxyethoxy)​-​3, ​5-​dimethylphenyl]​-​5, ​7-​dimethoxy-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST, INHIBITOR

Mechanism of action

Antagonist of bromodomain containing 2;Antagonist of bromodomain containing 3;Inhibitor of bromodomain containing 3;Antagonist of bromodomain containing 4

Names and Identifiers

• Isomeric SMILES: CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2
• Molecular Weight: 370.4
• Reaxy-Rn: 18444347
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18444347&ln=

Associated Targets(Human)

BRD4 Tchem Bromodomain-containing protein 4 (19 Activities)

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRDT Tchem Bromodomain testis-specific protein (2 Activities)

Discover Target: BRDT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD3 Tchem Bromodomain-containing protein 3 (9 Activities)

Discover Target: BRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD2 Tchem Bromodomain-containing protein 2 (7 Activities)

Discover Target: BRD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)