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RVX-208
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| Category | Human immunodeficiency Virus (HIV) |
| CAS | 1044870-39-4 |
| Description | RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. Using binding assays and X-ray crystallography, we now show that RVX-208 selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. siRNA experiments further suggest that induction of ApoA-I mRNA is mediated by BET family member BRD4. These data indicate that RVX-208 increases ApoA-I production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. |
Product Information
| Synonyms | RVX208; RVX 208; RVX-208; Apabetalone. |
| IUPAC Name | 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-3H-quinazolin-4-one |
| Molecular Weight | 370.40 |
| Molecular Formula | C20H22N2O5 |
| Canonical SMILES | CC1=CC(=CC(=C1OCCO)C)C2=NC(=O)C3=C(C=C(C=C3N2)OC)OC |
| InChI | InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24) |
| InChIKey | NETXMUIMUZJUTB-UHFFFAOYSA-N |
| Purity | >98% |
| Density | 1.3±0.1 g/cm3 |
| Solubility | In Vitro: DMSO : ≥ 33 mg/mL(89.09 mM) In Vivo: 1.Add each solvent one by one:10% DMSO >> 40%PEG300 >> 5%Tween-80 >> 45% saline Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution 2.Add each solvent one by one:10% DMSO >> 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution 3.Add each solvent one by one:10% DMSO >> 90%corn oil Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution 4.Add each solvent one by one:5% DMSO >> 40%PEG300 >> 5%Tween-80 >> 50% saline Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution 5.Add each solvent one by one:5% DMSO >> 95% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution 6.Add each solvent one by one:1% DMSO >> 99% saline Solubility: ≥ 0.5 mg/mL (1.35 mM); Clear solution |
| Appearance | white solid powder |
| Storage | Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month |
| Complexity | 543 |
| Exact Mass | 370.152863 |
| Index Of Refraction | 1.596 |
| In Vitro | In AGMs, Apabetalone was able to significantly increase serum apoA-I and HDL-C while increasing cholesterol outflow through multiple routes. |
| In Vivo | In vitro experiments, Apabetalone is able to activate apolipoprotein AI gene expression, increasing apoA-I and HDL-C. RVX-208 is capable of inhibiting BET bromine domain proteins and preferentially binds to the second bromine domain protein of BET proteins. |
| PSA | 93.67000 |
| Target | BD2 (Cell-free assay) |
| XLogP3-AA | 2.3 |
