| CAS NO: | 1044870-39-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 370.4 |
|---|---|
| Formula | C20H22N2O5 |
| CAS No. | 1044870-39-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 74 mg/mL (199.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | 0.5% CMC Na (1N HCl, PH 2.5-3.0): 8 mg/mL |
| Synonyms | RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone. Chemical Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one InChi Key: NETXMUIMUZJUTB-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3 |
| In Vitro | In vitro activity: As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. Kinase Assay: Experiments are run on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. IC50 values are calculated in Prism 5 after normalization against corresponding DMSO controls. Assays are performed according to the manufacturer’s protocol with minor modifications. Cell Assay: HepG2 cells treated with RVX-208 (5 μM) for 4 h only modestly affected BET-dependent gene transcription. Moreover, RVX-208 increased apolipoprotein (apo)A-I and high-density lipoprotein cholesterol (HDL-C) levels in HepG2 cells. |
|---|---|
| In Vivo | RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. |
| Animal model | Naive adult male AGMs |
| Formulation & Dosage | Dissolved in 1N HCl and carboxymethyl cellulose; 60mg/kg; i.v. injection or p.o. |
| References | Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9; Curr Opin Investig Drugs. 2010 Mar;11(3):357-64; J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9. |
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