| Identification | Back Directory | [Name]
RVX-208 | [CAS]
1044870-39-4 | [Synonyms]
CS-686
CS-1815
RVX-208
RVX-000222
Apabetalone
RVX-208 USP/EP/BP
RVX-208(RVX000222)
Apabetalone-RVX-208
RVX-208(RVX 000222)
APABETALONE; RVX-000222; RVX208; RVX 208; RVX000222; RVX 000222
2-(4-(2-hydroxyethoxy)-3,5-diMethylphenyl)-5,7-diMethoxyquinazolin-4(3H)-one
4(3H)-Quinazolinone, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone RVX-208 | [Molecular Formula]
C20H22N2O5 | [MDL Number]
MFCD18633270 | [MOL File]
1044870-39-4.mol | [Molecular Weight]
370.399 |
| Chemical Properties | Back Directory | [Boiling point ]
594.2±60.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C (des.) | [solubility ]
Soluble in DMSO (up to 75 mg/ml) or in Ethanol (up to 4 mg/ml). | [form ]
solid | [pka]
14.21±0.10(Predicted) | [color ]
White | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription.1 The human BET proteins contain two bromodomains, the first (BD1) being closer to the N-terminus than the second (BD2). RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 μM) over BD1 (IC50 = 1.8-3.1 μM).2,3 RVX-208 causes the selective release of BET proteins from chromatin in cells.2,3 It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans.4,5 RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.5 | [Uses]
RVX-208 is a selective antagonist of bromodomain and extra terminal (BET)’s bromodomains. | [target]
BD2 | [References]
1) Picaud?et al. (2013),?RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain; Proc. Natl. Acad. Sci. USA,?110?19754
2) McLure?et al. (2013),?RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist; PLoS One,?8e83190
3) Bailey?et al. (2010),?RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; J. Am. Coll. Cardiol.,?55?2580
4) Jahagirdar?et al. (2014),?A novel BET bromodomain inhibitor, RVX-208 shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice; Atherosclerosis,?236?91 |
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