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Technical Data
| Formula | C24H16F3N5 |
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| 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 | |||
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* <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.) |
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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. | ||
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| Targets |
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| 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] |
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References
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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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.