RVX-208

Catalog No.S7295

RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.

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RVX-208 Chemical Structure

RVX-208 Chemical Structure
Molecular Weight: 370.4

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.
Targets BD2 [1]
(Cell-free assay)
IC50 0.51 μM
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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HepG2MkfzSpVv[3Srb36gZZN{[Xl?MlLMglYxKM7:TR?=NFe0cJJFVVORNVm1dY9XcW6mdXPld{BieG:DLVmgcXJPSSCjbnSg[IUhdm:4bzDzfY51cGW|aYOgc4Yh[XCxQT3JMi=>NH3tOYMzODVzM{W5PS=>
U2OSM1\pO2Z2dmO2aX;uJIF{e2G7MWT+OUDPxE1?M3TwRoRqe3CuYXPld{BDTVRicILveIVqdnNiZoLvcUBkcHKxbXH0bY4>MYOyOFI1QDN5OR?=

... Click to View More Cell Line Experimental Data

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.

Animal Study:

[3]

Animal Models Naïve adult male AGMs
Formulation 1N hydrochloride and carboxymethyl cellulose
Dosages ~60 mg/kg
Administration Oral gavage or intravenous administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Picaud S, et al. Proc Natl Acad Sci U S A. 2013, 110(49), 19754-19759.

[2] McNeill E. Curr Opin Investig Drugs. 2010, 11(3), 357-364.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02586155 Recruiting Diabetes Mellitus, Type 2|Coronary Artery Disease|Cardiovascular Diseases Resverlogix Corp|PPD|ICON plc|Medidata Solutions October 2015 Phase 3
NCT01863225 Terminated Dyslipidemia|Coronary Artery Disease Resverlogix Corp|South Australian Health and Medical Rese  ...more Resverlogix Corp|South Australian Health and Medical Research Institute May 2013 Phase 2
NCT01728467 Completed Diabetes Resverlogix Corp|Baker IDI Heart and Diabetes Institute|N  ...more Resverlogix Corp|Baker IDI Heart and Diabetes Institute|Nucleus Network Ltd November 2012 Phase 2
NCT01067820 Completed Coronary Artery Disease Resverlogix Corp|The Cleveland Clinic September 2011 Phase 2
NCT01423188 Completed Coronary Artery Disease|Dyslipidemia Resverlogix Corp|The Cleveland Clinic August 2011 Phase 2

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Chemical Information

Download RVX-208 SDF
Molecular Weight (MW) 370.4
Formula

C20H22N2O5

CAS No. 1044870-39-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms RVX-000222
Solubility (25°C) * In vitro DMSO 74 mg/mL (199.78 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 0.5% CMC Na (1N HCl, PH 2.5-3.0) 8mg/mL
* <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-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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