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AZD3839

AZD3839 1227163-56-5
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Chemical Information
Product name:AZD3839 Purity:98% min
CAS NO:1227163-56-5 Solubility:10 mM in DMSO
Molecular Formula:C24H15F4N5 Package:Package according to customer requirements
Molecular Weight:449.403 Storage:Store at -20℃
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Remarks

AZD3839 is a potent and selective BACE1 inhibitor. AZD3839 is clinical candidate for the treatment of Alzheimer disease. AZD3839 inhibits BACE1 activity, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from mouse and guinea pig primary cortical neurons. Selectivity against BACE2 and cathepsin D was 14 and >1000-fold, respectively. AZD3839 exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 effectively reduces the levels of Aβ in brain, CSF, and plasma in several preclinical species.


References

1: Sparve E, Quartino AL, Lüttgen M, Tunblad K, Gårdlund AT, Fälting J, Alexander R, Kågström J, Sjödin L, Bulgak A, Al-Saffar A, Bridgland-Taylor M, Pollard C, Swedberg MD, Vik T, Paulsson B. Prediction and modeling of effects on the QTc interval for clinical safety margin assessment, based on single-ascending-dose study data with AZD3839. J Pharmacol Exp Ther. 2014 Aug;350(2):469-78. doi: 10.1124/jpet.114.215202. Epub 2014 Jun 10. PubMed PMID: 24917547.

2: Lindgren A, Eklund G, Turek D, Malmquist J, Swahn BM, Holenz J, von Berg S, Karlström S, Bueters T. Biotransformation of two β-secretase inhibitors including ring opening and contraction of a pyrimidine ring. Drug Metab Dispos. 2013 May;41(5):1134-47. doi: 10.1124/dmd.112.050351. Epub 2013 Mar 8. PubMed PMID: 23474650.

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