Antibodies
RVX-208
- 貨號 Cat. No.
- S7295
- 規格 Size
- 5mgã€20 mg
- 品牌 Brand
- Selleckchem
Description
RVX-208
Catalog No.S7295
RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2, about 170-fold selectivity over BD1. Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2, about 170-fold selectivity over BD1. Phase 2. | |||||
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| Targets | BD2 | |||||
| IC50 | 0.510 μM[1] | |||||
| In vitro | As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. [1] RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. [2] [3] | |||||
| In vivo | RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3] | |||||
| Features | First-in-class BD2-selective inhibitor of BET bromodomain and has been tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Competitive Histone Displacement Assay (AlphaScreen 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. |
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Animal Study: [3]
| Animal Models | Naïve adult male AGMs |
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| Dosages | ~60 mg/kg |
| Administration | Oral gavage or intravenous administration |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01058018 | Completed | Atherosclerosis|Coronary Artery Disease | Resverlogix Corp | 2009-12 | Phase 2 |
| NCT01423188 | Completed | Coronary Artery Disease|Dyslipidemia | Resverlogix Corp|The Cleveland Clinic | 2011-08 | Phase 2 |
| NCT01067820 | Completed | Coronary Artery Disease | Resverlogix Corp|The Cleveland Clinic | 2011-09 | Phase 2 |
| NCT01728467 | Recruiting | Diabetes | Resverlogix Corp|Baker IDI Heart and Diabetes Institute|Nucleus Network Ltd (local sponsor) | 2012-11 | Phase 2 |
| NCT01863225 | Terminated | Dyslipidemia|Coronary Artery Disease | Resverlogix Corp|South Australian Health and Medical Research Institute | 2013-05 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 370.4 |
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| Formula | C20H22N2O5 |
| CAS No. | 1044870-39-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | RVX-000222 |
| Solubility (25°C) * | In vitro | DMSO | 74 mg/mL (199 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 4(3H)​-​Quinazolinone, 2-​[4-​(2-​hydroxyethoxy)​-​3,​5-​dimethylphenyl]​-​5,​7-​dimethoxy- |
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