In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension
5% dimethylacetamide
20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid,pH 3
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
2.000mg/ml
(4.64mM)
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 (Cell-free assay)
26.1 nM(Ki)
In vitro
In SH-SY5Y cells, AZD3839 efficiently decreases the A
40 levels with IC50 of 4.8 nM, and decreases the formation of sAPP
with IC50 of 16.7 nM. This compound also decreases the A
40 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. It causes in vitro BACE1 inhibition in the cell assay with IC50 value of 16.7 nM.
In Vivo
In C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain A
. In guinea pig and non-human primates, this compound also inhibits A
generation.
A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy
[ Analyst, 2022, 10.1039/d2an00031h]
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]
Multiple BACE1 inhibitors abnormally increase the BACE1 protein level in neurons by prolonging its half-life.
[ Alzheimers Dement, 2019, 15(9):1183-1194]
Elevated cleavage of neuregulin-1 by beta-secretase 1 in plasma of schizophrenia patients.
[ Prog Neuropsychopharmacol Biol Psychiatry, 2019, 90:161-168]
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]
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.
