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| 品牌 | absin | CAS | 612487-72-6 |
|---|---|---|---|
| 分子式 | C19H18N4O2 | 纯度 | ＞98% |
| 分子量 | 334.37 | 货号 | abs810379 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a selective, orally active, brain pe | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
AZD1080 612487-72-6
| 产品描述 | |
| 描述 | AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | AZD 1080,AZD-1080 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 52 mg/mL (155.51 mM) |
| 生物活性 | |
| 靶点 | GSK-3α ,GSK-3β |
| In vitro(体外研究) | AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with a Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against cdk2, cdk5, cdk1 and Erk2. AZD1080 inhibits tau phosphorylation in cells expressing human tau, with IC50 of 324 nM. |
| In vivo(体内研究) | AZD1080 inhibits tau phosphorylation in rat brain after oral dministration, with brain/plasma exposure ratio of 0.5 – 0.8 at peak concentrations. AZD1080 reverses cognitive deficits and rescues dysfunctional synapses in mice. Acute oral treatment with AZD1080 inhibits peripheral GSK3 activity, produces a dose-dependent reduction of the phosphorylated to total glycogen synthase (GS) ratio, with a mean maximal inhibitory effect of 49% at the highest dose (10 μmol/kg) at 2 h after dosing. |
| 研究领域 | |
| 研究领域 | Stem CellsSignaling Pathways Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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