AZD3839 free base

SKU: orb1300481

Description

AZD3839 free base is a potent and selective BACE1 inhibitor (Ki = 26.1 nM) with 14-fold selectivity versus BACE2. This compound has been evaluated in Phase 1 clinical trials and serves as a research tool for Alzheimer's disease studies in biochemical and cellular assays.

Research Area

Neuroscience

Key Properties

• CAS Number: 1227163-84-9
• MW: 431.41
• Purity: 99.96%
• Formula: C₂₄H₁₆F₃N₅
• SMILES: NC1=N[C@@](c2cccc(F)c12)(c1cccc(c1)-c1cncnc1)c1ccnc(c1)C(F)F
• Target: Beta-Secretase,BACE
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.65 mM);DMSO:80 mg/mL (185.44 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:80 mg/mL (185.44 mM)

Bioactivity

• Target IC50:
  BACE1:26.1 nM(Ki)
• In Vivo:
  In C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation.
• In Vitro:
  In SH-SY5Y cells, AZD3839 efficiently decreases the Aβ40 levels with IC50 of 4.8 nM, and decreases the formation of sAPPβ with IC50 of 16.7 nM. AZD3839 also decreases the Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons with IC50 values of 50.9, 32.2, and 24.8 nM, respectively. AZD3839 causes in vitro BACE1 inhibition in the cell assay with IC50 value of 16.7 nM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

βSecretase, β-Secretase, BetaSecretase, Beta-secretase, b-Secretase, bSecretase, BACE, AZD3839, AZD-3839, AZD3839 free base, AZD-3839 free base, AZD 3839

Compound Identifiers

PubChem CID

46202416