Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WAY262611是一种 Wnt/β- 联蛋白激动剂,也是一种Dkk1的抑制剂。它能够增加骨形成速率,在 TCF- 荧光素酶测定实验中的EC50=0.63 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 238 | 现货 | ||
5 mg | ¥ 592 | 现货 | ||
10 mg | ¥ 788 | 现货 | ||
25 mg | ¥ 1,570 | 现货 | ||
50 mg | ¥ 2,980 | 现货 | ||
100 mg | ¥ 4,320 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 666 | 现货 |
产品描述 | WAY262611 is a Wnt/β-catenin agonist and an inhibitor of Dkk1. It increases bone formation rate with EC50 of 0.63 μM in TCF-luciferase assay. |
靶点活性 | β-Catenin(in TCF-Luciferase assay):0.63 μM |
体外活性 | WAY-262611 has the most potent activity, low kinase inhibition potential, and high solubility in the primary assay[1]. |
体内活性 | WAY-262611 has excellent pharmacokinetic properties and shows a increase in the trabecular bone formation rate in ovariectomized rats following oral administration in a dose-dependent manner. Calvariae from wt mice treated with WAY-262611 shows statistically increased BFR, but similarly treated KO animals are no different from control. This indicates that WAY-262611 is acting via the Wnt β-catenin pathway and most likely through inhibition of Dkk-1[1]. |
激酶实验 | PI3K and mTOR kinase assay : Enzyme assays are done in fluorescent polarization (FP) format, adapted from the Echelon K-1100 PI3K FP assay kit protocol. Human class I PI3Ks and PI3K-α mutants (E545K and H1047R) are produced in Sf9 or purchased from Upstate Biotech. GST-GRP1 (murine) is produced in Escherichia coli and isolated by GST-Sepharose. Assay buffers are reaction buffer [20 mM HEPES (pH 7.1), 2 mM MgCl2, 0.05% CHAPS, and 0.01% β-mercaptoethanol] and stop/detection buffer [100 mM HEPES (pH 7.5), 4 mM EDTA, 0.05% CHAPS]. FP reaction is run for 30 minutes at room temperature in 20 μL of reaction buffer containing 20 μM phosphatidylinositol 4,5-bisphosphate (PIP2), 25 μM ATP, and <4% DMSO. FP reaction is stopped with 20 μL of stop/detection buffer (10 nM probe and 40 nM GST-GRP), and after 2 hours, data are collected using an Envision plate reader. The routine assays with purified FLAG-TOR (FL and 3.5) are performed in 96-well plates as follows. Enzymes are first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 μM microcystin LR, and 100 μg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL test inhibitor or control vehicle dimethyl sulfoxide (DMSO). The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-TOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1–6 hours) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). |
分子量 | 318.42 |
分子式 | C20H22N4 |
CAS No. | 1123231-07-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 42 mg/mL (131.90 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1405 mL | 15.7025 mL | 31.4051 mL | 78.5127 mL |
5 mM | 0.6281 mL | 3.1405 mL | 6.281 mL | 15.7025 mL | |
10 mM | 0.3141 mL | 1.5703 mL | 3.1405 mL | 7.8513 mL | |
20 mM | 0.157 mL | 0.7851 mL | 1.5703 mL | 3.9256 mL | |
50 mM | 0.0628 mL | 0.3141 mL | 0.6281 mL | 1.5703 mL | |
100 mM | 0.0314 mL | 0.157 mL | 0.3141 mL | 0.7851 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。
WAY-262611 1123231-07-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Beta catenin Inhibitor β-catenin WAY 262611 inhibit WAY262611 inhibitor