EOS Med Chem produce Apabetalone 1044870-39-4, assay 99.2% to be China biggest, NMR, MS, COA is OK.
2017 China CPHI: E1M35
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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.
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