AZD3839

Catalog No.S7731

AZD3839 Chemical Structure

Molecular Weight(MW): 431.41

AZD3839 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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Biological Activity

Description AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
Targets
BACE1 [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y cells NUiweVl{TnWwY4Tpc44h[XO|YYm= M3fZeVE3KGh? NFHZWI5KdmirYnn0bY9vKG:oIFLBR2UyKGmwIHj1cYFvKFOKLWPZOXkh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDzRXBR[mW2YTDy[Yxm[XOnIHHmeIVzKDF4IHjyd{BjgSCrbX31co9ie3OjeTygTWM2OD1yLkCxOlch|ryP M4D3VFIzQTJ2OEG1
CHO cells M4j5ZmZ2dmO2aX;uJIF{e2G7 MlTwTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSCLb37Xc5JseyCjc4PhfUwhUUN3ME20Mlgh|ryP M{jNcFIzQTJ2OEG1

... Click to View More Cell Line Experimental Data

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]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: 5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3.
  • Dosages: 69 mg/kg daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.34 mM)
Ethanol 86 mg/mL warmed (199.34 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 431.41
Formula

C24H16F3N5

CAS No. 1227163-84-9
Storage powder
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01348737 Completed Alzheimers Disease|Safety|Tolerability|Blood Concentration|Healthy Volunteers AstraZeneca June 2011 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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BACE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID