产品名称

RVX 208 - RVX 000222

产品货号

Axon 2245 CAS [1044870-39-4] MF C20H22N2O5MW 370.40 Purity: 100% Soluble in DMSO Description BET bromodomain inhibitor specific for second bromodomains (BD2s), currently in phase I/II clinical trials for the treatment of cardiovascular diseases (IC50 values of 87 and 0.51 μM derived from the AlphaScreen data on BRD3 BD1 and BD2 resp.). RVX 208 preferentially binds to the second bromodomain found on BET proteins, exhibiting selectivity over BD1 of up to 23-fold with a KD of 195 nM against BD2 and 4 μM against BD1 of BRD3. RVX 208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner, and leads to an increase of plasma levels of the high-density lipid protein ApoA1, wich has emerged as a promising approach for the treatment of atherosclerosis. References Certificates Categories Extra info S. Picaud et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc. Natl. Acad. Sci. U.S.A. 2013, 110, 19754-19759. K.G. McLure et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013, 8, e83190. E. McNeill, Eileen. RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases. Curr. Opini. Invest. Drugs. 2010, 11, 357-364. Certificate of Analysis Material Safety Data Sheet Cardiovascular Cell Signaling & Oncology CNS Epigenetics BET (BRD) BET bromodomain inhibitor specific for second bromodomains (BD2s) Chemical name 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one Parent CAS No. [1044870-39-4] Order Size Unit Price Stock 2 mg €65.00 In Stock

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axonmedchem

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RVX 208 - RVX 000222

Based on 18 reference(s) in Google Scholar 9 10 18

Axon 2245

CAS [1044870-39-4]

MF C20H22N2O5
MW 370.40

Purity: 100%
Soluble in DMSO

RVX 208

Description

BET bromodomain inhibitor specific for second bromodomains (BD2s), currently in phase I/II clinical trials for the treatment of cardiovascular diseases (IC50 values of 87 and 0.51 μM derived from the AlphaScreen data on BRD3 BD1 and BD2 resp.). RVX 208 preferentially binds to the second bromodomain found on BET proteins, exhibiting selectivity over BD1 of up to 23-fold with a KD of 195 nM against BD2 and 4 μM against BD1 of BRD3. RVX 208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner, and leads to an increase of plasma levels of the high-density lipid protein ApoA1, wich has emerged as a promising approach for the treatment of atherosclerosis.