AZD3839 (1227163-84-9) Description
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. target: BACE1, β-secretase enzyme  IC50: 23.6 uM  AZD3839 dissolved in 0.33% dimethylsulfoxide In vitro: AZD3839 and its metabolites M1 and M2 inhibited CYP3A4 in a reversible and an irreversible manner, which could affect not only the metabolism of other CYP3A4 substrates but also the metabolism of AZD3839 itself.  In vivo: AZD3839 is dissolved in 0.3 M gluconic acid, adjusted to pH 3. Solutions of 0.75, 2.5, and 7.5 mg/ml are prepared and are administered orally by gavage at 2 ml body weight at 1.5, 5, and 15 mg (study 1) and 15 mg (study 2). AZD3839 effectively reduces the levels of Aβ in brain, CSF, and plasma in several preclinical species.
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.
AZD3839 (1227163-84-9) Specifications
|Synonym||AZD3839; AZD-3839; AZD 3839.|
|Purity||≥ >98% (or refer to the Certificate of Analysis)|
|Monoisotopic Mass||431.136 g/mol|
|Solubility||Soluble in DMSO|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months)|
|Shelf life||> >2 years if stored properly|
|Handling||Protect from air and light|
|Application||AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.|