RVX-208

Aliases: 2-{4-(2-hydroxyethoxy)-3,5-dimethylphenyl}-5,7-dimethoxy-4(3H)-quinazolinone
Catalog No: 14090 Format: 25 mg ¥66,000 Buy
Catalog No: 14091 Format: 5 mg ¥20,000 Buy

Application: Bromodomains

Chemical Properties

MW = 370.4
C20H22N2O5
CAS 1044870-39-4
>98% (TLC); NMR (Conforms)

Description

RVX-208 is a potent BET bromodomain antagonist with (IC50 = 0.51 µM for BD2) with approximately 170-fold selectivity over BD1 (ref 1,2). Increases apolipoprotein A-1 and HDL cholesterol in vitro and in vivo (ref 3). Reduces atherosclerosis (ref 4).

Contents

White powder. May be dissolved in DMSO (75 mg/ml); Ethanol (4 mg/ml).

Storage Conditions

Store desiccated as supplied at -20°C for up to 2 years. Store solutions at -20°C for up to 1 month.

References

1. S Picaud et al. Proc. Natl. Acad. Sci. USA 2013, 110:19754
2. KG McLure et al. PLoS One 2013, 8:e83190
3. D Bailey et al. J. Am. Coll. Cardiol. 2010, 55:2580
4. R Jahagirdar et al. Atherosclerosis 2014, 236:91

 

Chemical structure of RVX-208.