RVX-208, BET Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60177-2S 2 mg solid $79
M60177-10S 10 mg solid $316

Description

Product Information
Molecular Weight: 370.40
Formula: C20H22N2O5
Purity: ≥98%
CAS#: 1044870-39-4
Solubility: DMSO up to 100 mM
Chemical Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

RVX-208 is a potent and selective BET bromodomain inhibitor with an IC50 of 0.51 μM for the second bromodomain (BD2), which is about 170-fold selectivity over BD1. RVX 208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner, increases apoA-I and HDL-C in vitro and in vivo. In AGMs, RVX-208 raises serum pre-beta(1)-LpA-I and alpha-LpA-I levels and enhances cholesterol efflux. RVX-208 is the first-in-class BD2-selective inhibitor of BET bromodomain tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis.

 


How to Use:

 

 

  • In vitro: RVX-208 was used at 10 µM final concentration in various in vitro assays.
  • In vivo: RVX-208 was dosed to naïve adult male African green monkeys (AGMs) by oral gavage or intravenous administration at 60 mg/kg once per day.

 

 

 

Reference:

 

  1. Bailey D, et al. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. (2010) J Am Coll Cardiol. 55(23):2580-9.
  2. Picaud S, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. (2013) Proc Natl Acad Sci USA. 110(49):19754-9.
  3. McLure KG, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. (2013) PLoS One. 8(12):e83190.


 

Products are for research use only. Not for human use.

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