product name AZD3839
Description: AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, it is about 14-fold selectivity over BACE2. AZD3839 is clinical candidate for the treatment of Alzheimer disease. It inhibits BACE1 activity, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from mouse and guinea pig primary cortical neurons. AZD3839 exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate.
References: J Biol Chem. 2012 Nov 30;287(49):41245-57; J Med Chem. 2012 Nov 8;55(21):9346-61.
431.41
Formula
C24H16F3N5
CAS No.
1227163-84-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 86 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 86 mg/mL (199.3 mM)
Solubility (In vivo)
5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3: 2 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399841
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: AZD3839 concentration-dependently inhibited BACE1 activity in a biochemical fluorescence resonance energy transfer assay, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from guinea pig and mouse primary cortical neurons. Selectivity against BACE2 and cathepsin D was 14 and >1000-fold, respectively. |
|---|---|
| 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. |
| Animal model | C57BL/6 mice. |
| Formulation & Dosage | Dissolved in 5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3.; 69 mg/kg; p.o. administration |
| References | J Biol Chem. 2012 Nov 30;287(49):41245-57; J Med Chem. 2012 Nov 8;55(21):9346-61. |
Related Posts
product name AZD3839
Description: AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, it is about 14-fold selectivity over BACE2. AZD3839 is clinical candidate for the treatment of Alzheimer disease. It inhibits BACE1 activity, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from mouse and guinea pig primary cortical neurons. AZD3839 exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate.
References: J Biol Chem. 2012 Nov 30;287(49):41245-57; J Med Chem. 2012 Nov 8;55(21):9346-61.
431.41
Formula
C24H16F3N5
CAS No.
1227163-84-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 86 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 86 mg/mL (199.3 mM)
Solubility (In vivo)
5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3: 2 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399841
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: AZD3839 concentration-dependently inhibited BACE1 activity in a biochemical fluorescence resonance energy transfer assay, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from guinea pig and mouse primary cortical neurons. Selectivity against BACE2 and cathepsin D was 14 and >1000-fold, respectively. |
|---|---|
| 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. |
| Animal model | C57BL/6 mice. |
| Formulation & Dosage | Dissolved in 5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3.; 69 mg/kg; p.o. administration |
| References | J Biol Chem. 2012 Nov 30;287(49):41245-57; J Med Chem. 2012 Nov 8;55(21):9346-61. |