Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD2858 是具有口服活性的GSK-3抑制剂,可以抑制 GSK-3α (IC50:0.9 nM) 和 GSK-3β (IC50:5 nM) 的活性,可用于骨折愈合的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 257 | 现货 | ||
2 mg | ¥ 361 | 现货 | ||
5 mg | ¥ 575 | 现货 | ||
10 mg | ¥ 927 | 现货 | ||
25 mg | ¥ 1,850 | 现货 | ||
50 mg | ¥ 3,480 | 现货 | ||
100 mg | ¥ 4,960 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 986 | 现货 |
产品描述 | AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway. |
靶点活性 | GSK-3:68 nM |
体外活性 | 30 μM/kg AZD2858处理大鼠三周后胼胝中矿物质密度(2周时28%,三周时38%)和矿物质含量(两周时81%,三周时93%)增加.大鼠用AZD2858处理28天后,血清中骨更新标志物产生时间依赖性变化,且骨密度增加.大鼠用AZD2858处理7天后,骨形成标志P1NP增加,溶蚀标志物TRAcP-5b降低,表明骨合成代谢增加,大鼠吸收减少.大鼠口服AZD2858治疗两周后,与对照组相比,引起骨密度剂量依赖增加,治疗两周后,在每天20 mg/kg(总BMC: 对照组的172%)剂量下具有最大疗效.AZD2858处理使骨折恢复更快,有骨性骨痂但没有明显的软骨成分. |
体内活性 | AZD2858在人类和大鼠间充质干细胞中引起β-连环蛋白稳定,激活体外成骨细胞和成骨矿化。初级分离的人成骨细胞样细胞上AZD2858处理(1 μM,12小时)导致β-连环蛋白水平增加3倍。 |
激酶实验 | Tau phosphorylation assay: NIH-3T3 cells expressing 4-repeat Tau are used to assess functional activity of AZD2858 in vitro. The cells are grown in DMEM media and 2 mM L-glut, and 10% HiFCS, and plated at a concentration of 6×105 cells/well in 6-well plates. In each experiment, AZD2858 is dosed in triplicates at a concentration of 1, 10, 100, 500, 1000, 2000 and 10,000 nM. Cells are treated for 4 h prior to cell lysis using 100 μL ice cold lysis buffer (0.5% NP-40, 10 mM Tris, pH 7.2, 150 mM NaCl, 2 mM EDTA). A suspension is made with addition of protease and phosphatase inhibitors: 50 mM NaF, 0.2 mM NaVO4 and Cocktail Protease inhibitors. The solution is then snap frozen at ? 80 °C for at least 1 h, before thawing on ice and lysate clarification by centrifugation, followed by Western blot according to standard protocols. After blocking, the blots are exposed to the primary antibody, Phospho-Ser396-tau (1:1000) over night, washed and incubated with the secondary antibody (donkey anti-rabbit, 1:5000), followed by a final wash. For re-probing, the primary antibody Tau5 (1:200) and the secondary horseradish peroxidase linked antibody (sheep anti-mouse, 1:10000) are used. All blots are developed using ECL Western blot detection reagents, Kodak X-ray films, quantified using densitometric analysis, and the ratio of S396 tau to total tau (tau5) is calculated. |
细胞实验 | Human adipose derived stem cells and rat MSCs (isolated from bone marrow of Sprague Dawley rats at less than 8 weeks after gestation) are cultured in a basal media of DMEM containing 5% FBS and 2 mM GlutaMax. Cells are seeded in basal media into 96-well plates (3–5000 cells/well) for 18 h before treatment with AZD2858 (0.3 nM to 20 mM). After 24 h, β-catenin stabilisation is measured.(Only for Reference) |
分子量 | 453.52 |
分子式 | C21H23N7O3S |
CAS No. | 486424-20-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 7 mg/mL (15.43 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.205 mL | 11.0249 mL | 22.0497 mL | 55.1244 mL |
5 mM | 0.441 mL | 2.205 mL | 4.4099 mL | 11.0249 mL | |
10 mM | 0.2205 mL | 1.1025 mL | 2.205 mL | 5.5124 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。
AZD2858 486424-20-8 PI3K/Akt/mTOR signaling Stem Cells GSK-3 AZD-2858 Glycogen synthase kinase 3 Glycogen synthase kinase-3 inhibit Inhibitor AZD 2858 inhibitor