(S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine Chemical Properties

Boiling point:

596.3±60.0 °C(Predicted)

Density 

1.41±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 125 mg/mL (289.75 mM; Need ultrasonic)

form 

Powder

pka

2.56±0.40(Predicted)

color 

White to off-white

(S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine Usage And Synthesis

Biological Activity

AZD3839 is a potent and selective BACE1 inhibitor (Ki = 26.1 nM/BACE1, 372.4 nM/BACE2, >25 μM/Cathepsin D by cell-free TR-FRET; hERG IC50 = 4.8 μM) th at effectively suppresses cellular BACE1 activity in neuron cultures (sAPPβ release IC50 = 16.7 nM/SH-SY5Y; Aβ40 release IC50 = 4.8 nM/SH-SY5Y AAP695wt, 32.2 nM/N2A, 24.8 nM/guinea pig cortical neurons, 51 nM/murine cortical neurons) and exhibits in vivo Aβ40-, Aβ42-, sAPPβ-reducing efficacy (80 & 160 μmol/kg mouse, p.o.; 100 & 200 μmol/kg guinea pigs, p.o., 2.5 & 20 μmol/kg cynomolgus monkeys, i.v.) with good pharmacokinetic properties and oral availability.

(S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine(1227163-84-9)Related Product Information

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