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Applications: Useful as a BET Bromodomain inhibitor.
Biological Activity: RVX-208 has been shown to have an IC50 = 0.510 µM for BD2, which is~170-fold selectivity over BD1.
CAS Number: 1044870-39-4
Description: RVX-028, also known as RVX-000222, is a potent BET bromodomain inhibitor. Itpreferentially binds to the second bromodomain on BET proteins. It also stimulatesapolipoprotein (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 serumapoA-I and HDL-C in monkeys.
Format: A crystalline solid
Purity: ≥98% by HPLC
Solubility: Solubility in DMSO is 74 mg/ml. Solubility in water and ethanol is <1 mg/ml.
Storage Stability: Store at or below -20°C for up to two years.
Biosafety Level: Not applicable (BSL-1)
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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