product name RVX-208
Description: RVX-208 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. RVX-208 binds to the acetyl-lysine binding pocket in a peptide-competitive way. In HepG2 cells, RVX-208 induced messenger ribonucleic acid and protein synthesis of apolipoprotein (apo)A-I. It is currently undergoing phase III clinical trials for the treatment of cardiovascular diseases.
References: Proc Natl Acad Sci U S A. 2013;110(49):19754-9; Curr Opin Investig Drugs. 2010;11(3):357-64.
370.4
Formula
C20H22N2O5
CAS No.
1044870-39-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
0.5% CMC Na (1N HCl, PH 2.5-3.0): 8 mg/mL
Synonyms
RVX-000222
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19419465
| In Vitro |
In vitro activity: 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. Kinase Assay: Experiments are run on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. IC50 values are calculated in Prism 5 after normalization against corresponding DMSO controls. Assays are performed according to the manufacturer’s protocol with minor modifications. Cell Assay: HepG2 cells treated with RVX-208 (5 μM) for 4 h only modestly affected BET-dependent gene transcription. Moreover, RVX-208 increased apolipoprotein (apo)A-I and high-density lipoprotein cholesterol (HDL-C) levels in HepG2 cells. |
|---|---|
| In Vivo | RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. |
| Animal model | Naïve adult male AGMs |
| Formulation & Dosage | Dissolved in 1N HCl and carboxymethyl cellulose; 60mg/kg; i.v. injection or p.o. |
| References | Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9; Curr Opin Investig Drugs. 2010 Mar;11(3):357-64; J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9. |
