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AZD3839 free base

Catalog No. T6772   CAS 1227163-84-9
Synonyms: AZD3839

AZD3839 free base is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

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AZD3839 free base Chemical Structure
AZD3839 free base, CAS 1227163-84-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 68.00
5 mg In stock $ 116.00
10 mg In stock $ 178.00
25 mg In stock $ 363.00
50 mg In stock Inquiry
1 mL * 10 mM (in DMSO) In stock $ 123.00
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Purity: 99.96%
Purity: 99.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AZD3839 free base is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
Targets&IC50 BACE1:26.1 nM(Ki)
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. [1] AZD3839 causes in vitro BACE1 inhibition in the cell assay with IC50 value of 16.7 nM. [2]
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. [1]
Synonyms AZD3839
Molecular Weight 431.41
Formula C24H16F3N5
CAS No. 1227163-84-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (185.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 80 mg/mL (185.4 mM)

TargetMolReferences and Literature

1. Jeppsson F, et al. J Biol Chem. 2012, 287(49), 41245-41257. 2. Swahn BM, et al. J Med Chem. 2012, 55(21), 9346-9361.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Covalent Inhibitor Library Clinical Compound Library Drug Repurposing Compound Library NO PAINS Compound Library ReFRAME Related Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Inhibitor Library Anti-Hypertension Compound Library

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Keywords

AZD3839 free base 1227163-84-9 Neuroscience Beta-Secretase BACE AZD-3839 AZD 3839 β-Secretase AZD-3839 free base inhibit Beta-secretase Inhibitor AZD3839 inhibitor

 

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