2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile AZD1080
1H-Indole-5-carbonitrile, 2-hydroxy-3-[5-(4-morpholinylmethyl)-2-pyridinyl]-
CAS: 612487-72-6
Molecular Formula: C19H18N4O2
2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile AZD1080 - Names and Identifiers
2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile AZD1080 - Physico-chemical Properties
| Molecular Formula | C19H18N4O2 |
| Molar Mass | 334.37 |
| Density | 1.40±0.1 g/cm3(Predicted) |
| Boling Point | 594.0±50.0 °C(Predicted) |
| pKa | 8.32±0.50(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | AZD1080 is a selective, orally active, brain-permeable GSK3 inhibitor, inhibiting human GSK3α and GSK3β with K I values of 6.9 nM and 31 nM, respectively, showing a significant impact on CDK2,CDK5,> 14-fold selectivity for CDK1 and erk2. In cells expressing human tau protein, AZD1080 inhibits tau protein phosphorylation with an IC 50 of 324 nM.. |
| In vivo study | Oral administration of AZD1080 inhibited tau phosphorylation in rat brain, reaching a brain/plasma concentration ratio of 0.5-0.8 at the highest concentration. In mice, AZD1080 reversed cognitive deficits and rescued synaptic dysfunction. Acute oral administration of AZD1080 inhibited the activity of peripheral GSK3, resulting in a dose-dependent decrease in the ratio of phosphorylated glycogen synthase to total glycogen synthase (GS) at the highest dose (10 μmol/kg). The average maximum inhibition effect was 49%. |
2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile AZD1080 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.991 ml | 14.953 ml | 29.907 ml |
| 5 mM | 0.598 ml | 2.991 ml | 5.981 ml |
| 10 mM | 0.299 ml | 1.495 ml | 2.991 ml |
| 5 mM | 0.06 ml | 0.299 ml | 0.598 ml |
Last Update：2024-01-02 23:10:35
2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile AZD1080 - Reference Information
| bioactivity | AZD1080 is an orally active, selective, brain-permeable GSK3 inhibitor, inhibition of human GSK3α and GSK3β,Ki were 6.9 nM and 31 nM, respectively, more than 14 times higher than the effect on CDK2, CDK5, CDK1 and erk2. AZD1080 is an orally bioavailable, selective, brain-permeable GSK3 inhibitor that inhibits human GSK3α and GSK3β with a Ki of 6.9 nM and 31 nM, respectively, the selectivity of CDK2, CDK5, CDK1 and Erk2 was higher than 14 times. |
| features | A brain permeable GSK3 inhibitor. |
| Target | Value |
| GSK-3α (Cell-free assay) | 6.9 nM |
| GSK-3β (Cell-free assay) | 31 nM |
Last Update：2024-04-09 21:11:58
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Spot supply
Product Name: 1H-Indole-5-carbonitrile, 2-hydroxy-3-[5-(4-morpholinylmethyl)-2-pyridinyl]- Visit Supplier Webpage Request for quotationCAS: 612487-72-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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