Home Neuronal Signaling BACE inhibitor AZD3839 For research use only.

AZD3839

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

AZD3839 Chemical Structure

AZD3839 Chemical Structure

CAS No. 1227163-84-9

Purity & Quality Control

AZD3839 Related Products

Signaling Pathway

BACE Signaling Pathways

BACE Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y cells Function assay 16 h Inhibition of BACE1 in human SH-SY5Y cells assessed as inhibition of sAPPbeta release after 16 hrs by immunoassay, IC50=0.0167 μM 22924815
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by IonWorks assay, IC50=4.8 μM 22924815
Click to View More Cell Line Experimental Data

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 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 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]
Animal Research Animal Models C57BL/6 mice
Dosages 69 mg/kg daily
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01348737 Completed
Alzheimer''s Disease|Safety|Tolerability|Blood Concentration|Healthy Volunteers
AstraZeneca
 June 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 431.41 Formula

C24H16F3N5
CAS No. 1227163-84-9 SDF Download AZD3839 SDF
Smiles C1=CC(=CC(=C1)C2(C3=C(C(=CC=C3)F)C(=N2)N)C4=CC(=NC=C4)C(F)F)C5=CN=CN=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (199.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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