Cas No.: | 1227163-84-9 |
Chemical Name: | AZD3839 (free base) |
Synonyms: | AZD3839 (free base);AZD 3839 free base;AZD-3839 free base;AZD3839 free base |
SMILES: | FC1=C2C([C@](C3=CC=CC(C4=CN=CN=C4)=C3)(C5=CC(C(F)F)=NC=C5)N=C2N)=CC=C1 |
Formula: | C24H16F3N5 |
M.Wt: | 431.412554740906 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |
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/kg body weight at 1.5, 5, and 15 mg/kg (study 1) and 15 mg/kg (study 2). [1]AZD3839 effectively reduces the levels of Aβ in brain, CSF, and plasma in several preclinical species. [2] |
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. [1] |