RVX-208
Catalog #
27111
$230
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Description
RVX-028, also known as RVX-000222, is a potent BET bromodomain inhibitor. It preferentially binds to the second bromodomain on BET proteins. It also stimulates apolipoprotein (APO) AI gene expression, which increases apoA-I and HDL-C in vitro. In vivo, RVX-208 enhances cholesterol efflux via different pathways and significantly increases serum apoA-I and HDL-C in monkeys.
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Synonyms
RVX-000222
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Format
A crystalline solid
Formula
C20H22N2O5
MW
370.4 Da
Solubility
Solubility in DMSO is 74 mg/ml. Solubility in water and ethanol is <1 mg/ml.
Biological Activity
RVX-208 has been shown to have an IC50 = 0.510 μM for BD2, which is
~170-fold selectivity over BD1.
CAS Registry #
1044870-39-4
References
1. Bailey, D., et al., J Am Coll Cardiol. 2010;55(23):2580-2589.
2. Picaud, S., et al., Proc Natl Acad Sci U.S.A. 2013; 110(49):19754-19759.
3. McNeill, E. Curr Opin Investig Drugs. 2010;11(3):357-364.
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