Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD1080 是一种选择性GSK3抑制剂。它抑制重组人GSK3α和GSK3β,pKi(IC50) 分别为 8.2 (6.9 nM) 和 7.5 (31 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 281 | 现货 | ||
5 mg | ¥ 756 | 现货 | ||
10 mg | ¥ 1,263 | 现货 | ||
25 mg | ¥ 2,278 | 现货 | ||
50 mg | ¥ 3,798 | 现货 | ||
100 mg | ¥ 4,530 | 现货 | ||
500 mg | ¥ 9,720 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 553 | 现货 |
产品描述 | AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor. |
靶点活性 | GSK-3α:6.9 nM, GSK-3β:31 nM |
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。 |
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. |
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) |
分子量 | 334.37 |
分子式 | C19H18N4O2 |
CAS No. | 612487-72-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 49 mg/mL (146.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9907 mL | 14.9535 mL | 29.907 mL | 74.7675 mL |
5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL | 14.9535 mL | |
10 mM | 0.2991 mL | 1.4953 mL | 2.9907 mL | 7.4767 mL | |
20 mM | 0.1495 mL | 0.7477 mL | 1.4953 mL | 3.7384 mL | |
50 mM | 0.0598 mL | 0.2991 mL | 0.5981 mL | 1.4953 mL | |
100 mM | 0.0299 mL | 0.1495 mL | 0.2991 mL | 0.7477 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AZD1080 612487-72-6 PI3K/Akt/mTOR signaling Stem Cells GSK-3 AZD-1080 Glycogen synthase kinase-3 Glycogen synthase kinase 3 Inhibitor AZD 1080 inhibit inhibitor