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- CAS号：
612487-72-6
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/500mg
| 规格： | 1mg | 产品价格： | ￥240.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥442.0 |
| 规格： | 5mg | 产品价格： | ￥604.0 |
| 规格： | 10mg | 产品价格： | ￥1010.0 |
| 规格： | 25mg | 产品价格： | ￥1822.0 |
| 规格： | 50mg | 产品价格： | ￥3038.0 |
| 规格： | 100mg | 产品价格： | ￥3624.0 |
| 规格： | 500mg | 产品价格： | ￥7776.0 |
Product Introduction
Bioactivity
| 名称 | AZD1080 |
| 描述 | AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor. |
| 细胞实验 | 3T3 fibroblasts are engineered to stably express four-repeat tau protein. These cells have high endogenous levels of GSK3 that is able to phosphorylate tau protein constitutively. This phosphorylation is inhibited by LiCl. After treatment with different compounds, cultures are washed twice with 5 mM MgCl2-PBS. Extracts for Western blot analysis are prepared by homogenizing cells in ice-cold extraction buffer consisting of 20 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM NaF, 1% Triton X-100, 1 mM sodium orthovanadate, 10 mM EDTA, and protease inhibitors (2 mM phenylmethylsulfonyl fluoride, 10 μg/ml aprotinin, 10 μg/ml leupeptin, and 10 μg/ml pepstatin). The samples are homogenized at 4 °C, and protein content is determined by Bradford method. Total protein (25 μg) is electrophoresed on 10% SDS-PAGE gel and transferred to a nitrocellulose membrane. The experiments are performed using the following primary antibodies: tau Ser(P)-396, 1:1000; Tau5, 1:1000; and anti-GSK3β, 1:1000. The filters are incubated with the antibody at 4 °C overnight in 5% nonfat dried milk. A secondary antibody (1:5000), followed by ECL detection reagents are used for immunodetection. Quantitation of immunoreactivity is performed by densitometric scanning.(Only for Reference) |
| 激酶实验 | Kinase Assay: GSK3 scintillation proximity assay is done. The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μl and preincubated for 10–15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μl. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μl of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to 35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter. |
| 体外活性 | AZD1080逆转小鼠的认知缺陷并拯救其功能失调的突触.口服AZD1080抑制大鼠脑中tau蛋白磷酸化,在峰浓度下脑/血浆暴露比率为0.5-0.8.急性口服AZD1080抑制外围GSK3的活性,剂量依赖性降低磷酸化糖原合成酶和总糖原合成酶的比率,在最高剂量为10mol/kg时达到平均最大抑制效果49％. |
| 体内活性 | AZD1080抑制表达人类tau的细胞中的tau磷酸化,IC50为324 nM。AZD1080抑制人GSK3α和GSK3β,Ki 值分别为6.9 nM和31 nM,对cdk2、cdk5、cdk1和Erk2表现出> 14倍的选择性。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 40 mg/mL (119.63 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.98 mM), Sonication is recommended. |
| 关键字 | Inhibitor | inhibit | GSK-3β | GSK-3α | GSK-3 | GSK3 | Glycogen synthase kinase-3 | Glycogen synthase kinase 3 | AZD-1080 | AZD1080 | AZD 1080 |
| 相关产品 | Cromolyn sodium | ROCK-IN-5 | 4-Methyl-6-Methoxycoumarin | Ginsenoside Rg2 | 4-Chloro-2'-bromoacetophenone | AT7519 | (E/Z)-10-Hydroxy-2-decenoic acid | 5-Bromoindole | GSK-3 Inhibitor 5 | GSK 3 Inhibitor IX | Indazole | Ethyl linoleate |
| 相关库 | Inhibitor Library | Neuroprotective Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 AZD1080【612487-72-6】
￥240 - 7776
