AZD3839

Catalog No.S7731

For research use only.

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

CAS No. 1227163-84-9

Selleck's AZD3839 has been cited by 6 Publications

Purity & Quality Control

Choose Selective BACE Inhibitors

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 MmfVSpVv[3Srb36gZZN{[Xl? NIfFPHcyPiCq NYnNZWVIUW6qaXLpeIlwdiCxZjDCRWNGOSCrbjDoeY1idiCVSD3TXVV[KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gd2FRWGKndHGgdoVt\WG|ZTDh[pRmeiBzNjDodpMh[nliaX3teY5w[XO|YYmsJGlEPTB;MD6wNVY4KM7:TR?= MX2yNlkzPDhzNR?=
CHO cells NYHOOWdnTnWwY4Tpc44h[XO|YYm= NFPjUlVKdmirYnn0bY9vKG:oIHj1cYFvKEWURzDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IFnvcndwemu|IHHzd4F6NCCLQ{WwQVQvQCEQvF2= M4XQSlIzQTJ2OEG1
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 (from reference)

Animal Research:[1]
  • Animal Models: C57BL/6 mice
  • Dosages: 69 mg/kg daily
  • Administration: p.o.

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
(Data is from Selleck tests instead of citations):
5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3.
For best results, use promptly after mixing.

2mg/mL

Chemical Information

Molecular Weight 431.41
Formula

C24H16F3N5

CAS No. 1227163-84-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01348737 Completed Drug: AZD3839|Drug: AZD3839 Placebo Alzheimer''s Disease|Safety|Tolerability|Blood Concentration|Healthy Volunteers AstraZeneca June 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy AZD3839 | AZD3839 supplier | purchase AZD3839 | AZD3839 cost | AZD3839 manufacturer | order AZD3839 | AZD3839 distributor