EOS Med Chem produce Liraglutide（RVX-208） CAS:204656-20-2, assay 99.2% to be China biggest, NMR, MS, COA is OK.
2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
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Description: Apabetalone, also known as RVX-208, is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. RVX-208 may be a promising new approach to the treatment of atherosclerosis.
Name: Apabetalone
CAS#: 1044870-39-4
Chemical Formula: C20H22N2O5
Exact Mass: 370.15287
Molecular Weight: 370.39908
Elemental Analysis: C, 64.85; H, 5.99; N, 7.56; O, 21.60
Synonym: RVX208; RVX 208; RVX-208; Apabetalone.
IUPAC/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
TECHNICAL DATA
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
REFERENCES
1: Barylski M, Toth PP, Nikolic D, Banach M, Rizzo M, Montalto G. Emerging therapies for raising high-density lipoprotein cholesterol (HDL-C) and augmenting HDL particle functionality. Best Pract Res Clin Endocrinol Metab. 2014 Jun;28(3):453-61. doi: 10.1016/j.beem.2013.11.001. Epub 2013 Nov 15. PubMed PMID: 24840270.
2: 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. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013. PubMed PMID: 24391744; PubMed Central PMCID: PMC3877016.
3: 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. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PubMed PMID: 24248379; PubMed Central PMCID: PMC3856850.
4: Balder JW, Staels B, Kuivenhoven JA. Pharmacological interventions in human HDL metabolism. Curr Opin Lipidol. 2013 Dec;24(6):500-9. doi: 10.1097/MOL.0000000000000018. Review. PubMed PMID: 24184942.
5: Khmelnitsky YL, Mozhaev VV, Cotterill IC, Michels PC, Boudjabi S, Khlebnikov V, Madhava Reddy M, Wagner GS, Hansen HC. In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208). Eur J Med Chem. 2013 Jun;64:121-8. doi: 10.1016/j.ejmech.2013.03.062. Epub 2013 Apr 10. PubMed PMID: 23644195.
6: Joy TR. Novel HDL-based therapeutic agents. Pharmacol Ther. 2012 Jul;135(1):18-30. doi: 10.1016/j.pharmthera.2012.03.004. Epub 2012 Mar 23. Review. PubMed PMID: 22465158.
7: Nicholls SJ, Gordon A, Johannson J, Ballantyne CM, Barter PJ, Brewer HB, Kastelein JJ, Wong NC, Borgman MR, Nissen SE. ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies. Cardiovasc Drugs Ther. 2012 Apr;26(2):181-7. doi: 10.1007/s10557-012-6373-5. PubMed PMID: 22349989.
8: Rvx 208. Drugs R D. 2011;11(2):207-13. doi: 10.2165/11595140-000000000-00000. Review. PubMed PMID: 21679009; PubMed Central PMCID: PMC3585949.
9: Shah PK. Atherosclerosis: targeting endogenous apo A-I--a new approach for raising HDL. Nat Rev Cardiol. 2011 Apr;8(4):187-8. doi: 10.1038/nrcardio.2011.37. Epub 2011 Mar 1. PubMed PMID: 21364534.
10: Horowitz JD, Rosenson RS, McMurray JJ, Marx N, Remme WJ. Clinical Trials Update AHA Congress 2010. Cardiovasc Drugs Ther. 2011 Feb;25(1):69-76. doi: 10.1007/s10557-011-6285-9. PubMed PMID: 21340529.
11: Nicholls SJ, Gordon A, Johansson J, Wolski K, Ballantyne CM, Kastelein JJ, Taylor A, Borgman M, Nissen SE. Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial. J Am Coll Cardiol. 2011 Mar 1;57(9):1111-9. doi: 10.1016/j.jacc.2010.11.015. Epub 2011 Jan 20. PubMed PMID: 21255957.
12: Davidson MH. Apolipoprotein A-I therapy promise, challenges, and disappointment. J Am Coll Cardiol. 2011 Mar 1;57(9):1120-1. doi: 10.1016/j.jacc.2010.11.025. Epub 2011 Jan 20. PubMed PMID: 21255956.
13: Inazu A. [Novel therapy for atherosclerosis and inflammatory vascular disease]. Nihon Rinsho. 2011 Jan;69(1):105-9. Review. Japanese. PubMed PMID: 21226269.
