AZD3839 (free base)

AZD3839 is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 can be used in the field of Alzheimer's disease research[1][2][3].

Product Specifications

CAS Number

[1227163-84-9]

UNSPSC

12352005

Hazard Statement

H302

Target

Beta-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/AZD3839-free-base.html

Purity

99.97

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

FC1=C2C([C@](C3=CC=CC(C4=CN=CN=C4)=C3)(C5=CC(C(F)F)=NC=C5)N=C2N)=CC=C1

Molecular Formula

C24H16F3N5

Molecular Weight

431.41

Precautions

H302

References & Citations

[1]Sparve E et al. 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.|[2]Jeppsson F et al. Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem. 2012 Nov 30;287 (49) :41245-57.|[3]Eketjäll S, et al. AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics. J Alzheimers Dis. 2016;50 (4) :1109-23.