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RVX-208 CAS: 1044870-39-4

Category: Inhibitors
Product Name: RVX-208
Cat No: I000252
CAS No: 1044870-39-4
Synonyms: 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1H-quinazolin-4-one
Molecular Formula: C20H22N2O5
Molecular Weight: 370.4
SMILES: O=C1C2=C(OC)C=C(OC)C=C2NC(C3=CC(C)=C(OCCO)C(C)=C3)=N1
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
Solubility: DMSO: ≥ 33 mg/mL
Target: Bromodomain
Storage: Store at -20° C
CAS 1044870-39-4,RVX-208
  • Description

RVX-208(RVX 000222) is a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; is a BET bromodomain antagonist.
IC50 value:
Target: BET bromodomain antagonist
The RVX-208 induced apoA-I messenger ribonucleic acid and protein synthesis in HepG2 cells, leading to increased levels of pre-beta-migrating and alpha-lipoprotein particles containing apoA-I (LpA-I) in spent media. Similarly, in AGMs, RVX-208 treatment for 63 days increased serum apoA-I and HDL-C levels (60% and 97%, respectively) [1].
Like JQ-1, RVX-208 increased the Tm of all BET bromodomains, indicative of binding. RVX-208 competes for acetylated histone H4 peptide binding to both bromodomains of BRD4, similar to JQ-1, but with a preference for BD2 over BD1. RVX-208 also binds to the bromodomains of BRDs 2 and 3 with a similar preference for BD2 (KD~5–30 nM) over BD1 (KD~2–3 μM) [2].

  • Spec

Appearance:white solid powder
Purity: > 98%

  • References


1:RVX 208: a novel BET protein inhibitor, role as an inducer of apo A-I/HDL and beyond. Ghosh GC, Bhadra R, Ghosh RK, Banerjee K, Gupta A.Cardiovasc Ther. 2017 Apr 19. doi: 10.1111/1755-5922.12265. [Epub ahead of print] PMID: 28423226
2:Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes. Wasiak S, Gilham D, Tsujikawa LM, Halliday C, Norek K, Patel RG, McLure KG, Young PR, Gordon A, Kulikowski E, Johansson J, Sweeney M, Wong NC.Data Brief. 2016 Jul 29;8:1280-8. doi: 10.1016/j.dib.2016.07.047. eCollection 2016 Sep. PMID: 27570805 Free PMC Article
3:Corrigendum to "RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease" [Atherosclerosis 247 (2016) 48-57]. Gilham D, Wasiak S, Tsujikawa LM, Halliday C, Norek K, Patel RG, Kulikowski E, Johansson J, Sweeney M, Wong NC.Atherosclerosis. 2016 Oct;253:345. doi: 10.1016/j.atherosclerosis.2016.05.012. Epub 2016 May 20. No abstract available. PMID: 27211480 Free Article
4:Effects of the BET-inhibitor, RVX-208 on the HDL lipidome and glucose metabolism in individuals with prediabetes: A randomized controlled trial. Siebel AL, Trinh SK, Formosa MF, Mundra PA, Natoli AK, Reddy-Luthmoodoo M, Huynh K, Khan AA, Carey AL, van Hall G, Cobelli C, Dalla-Man C, Otvos JD, Rye KA, Johansson J, Gordon A, Wong NC, Sviridov D, Barter P, Duffy SJ, Meikle PJ, Kingwell BA.Metabolism. 2016 Jun;65(6):904-14. doi: 10.1016/j.metabol.2016.03.002. Epub 2016 Mar 8. PMID: 27173469
5:RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease. Gilham D, Wasiak S, Tsujikawa LM, Halliday C, Norek K, Patel RG, Kulikowski E, Johansson J, Sweeney M, Wong NC.Atherosclerosis. 2016 Apr;247:48-57. doi: 10.1016/j.atherosclerosis.2016.01.036. Epub 2016 Jan 22. PMID: 26868508 Free Article
6:Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial. Nicholls SJ, Puri R, Wolski K, Ballantyne CM, Barter PJ, Brewer HB, Kastelein JJ, Hu B, Uno K, Kataoka Y, Herrman JP, Merkely B, Borgman M, Nissen SE.Am J Cardiovasc Drugs. 2016 Feb;16(1):55-65. doi: 10.1007/s40256-015-0146-z. PMID: 26385396
7:An evaluation of RVX-208 for the treatment of atherosclerosis. Nikolic D, Rizzo M, Mikhailidis DP, Wong NC, Banach M.Expert Opin Investig Drugs. 2015;24(10):1389-98. doi: 10.1517/13543784.2015.1083010. Review. PMID: 26364508
8:A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Jahagirdar R, Zhang H, Azhar S, Tobin J, Attwell S, Yu R, Wu J, McLure KG, Hansen HC, Wagner GS, Young PR, Srivastava RA, Wong NC, Johansson J.Atherosclerosis. 2014 Sep;236(1):91-100. doi: 10.1016/j.atherosclerosis.2014.06.008. Epub 2014 Jun 28. PMID: 25016363
9:RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E, Suto RK, Wong NC, Wagner GS, Hansen HC, Young PR.PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PMID: 24391744 Free PMC Article
10:RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P.Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PMID: 24248379 Free PMC Article


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