AZD3839

Catalog No.S7731 Batch:S773103

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Technical Data

Formula

C24H16F3N5
Molecular Weight 431.41 CAS No. 1227163-84-9
Solubility (25°C)* In vitro DMSO 86 mg/mL (199.34 mM)
Ethanol 86 mg/mL (199.34 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
5% dimethylacetamide 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid,pH 3
2.0mg/ml Taking the 1 mL working solution as an example, take 2 mg of this product and add it to 1 ml of 5% dimethylacetamide+20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3 clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 Study:[1]
  • Animal Models

    C57BL/6 mice

  • Dosages

    69 mg/kg daily

  • Administration

    p.o.

Selleck's AZD3839 has been cited by 6 publications

A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy [ Analyst, 2022, 10.1039/d2an00031h] PubMed: 35253833
Identification and drug-induced reversion of molecular signatures of Alzheimer's disease onset and progression in AppNL-G-F, AppNL-F, and 3xTg-AD mouse models [ Genome Med, 2021, 13(1):168] PubMed: 34702310
Multiple BACE1 inhibitors abnormally increase the BACE1 protein level in neurons by prolonging its half-life. [ Alzheimers Dement, 2019, 15(9):1183-1194] PubMed: 31416794
Proteolytic Processing of Neuregulin 2. [ Mol Neurobiol, 2019, 10.1007/s12035-019-01846-9] PubMed: 31838721
Elevated cleavage of neuregulin-1 by beta-secretase 1 in plasma of schizophrenia patients. [ Prog Neuropsychopharmacol Biol Psychiatry, 2019, 90:161-168] PubMed: 30500411
Increased Foxo3a Nuclear Translocation and Activity is an Early Neuronal Response to βγ-Secretase-Mediated Processing of the Amyloid-β Protein Precursor: Utility of an AβPP-GAL4 Reporter Assay. [ J Alzheimers Dis, 0, 61(2):673-688] PubMed: 29254083

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.