[CAS NO. 1227163-84-9] AZD3839
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PRODUCTS SPECIFICATIONS [1227163-84-9]
Store
Catalog
SLK-S7731
Brand
Selleck
CAS
1227163-84-9
DESCRIPTION [1227163-84-9]
Overview
| MDL | MFCD25976574 |
|---|---|
| Molecular Weight | 431.41 |
| Molecular Formula | C24H16F3N5 |
| SMILES | NC1=N[C@@](C2=CC=CC(C3=CN=CN=C3)=C2)(C4=CC(C(F)F)=NC=C4)C5=C1C(F)=CC=C5 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
AZD3839 is a potent and selective inhibitor with 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. AZD3839 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 Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation.
References
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