Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD 9272 是一种脑渗透性的mGluR5 拮抗剂,可用于研究胃食管反流。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 623 | 现货 | ||
5 mg | ¥ 1,430 | 现货 | ||
10 mg | ¥ 2,120 | 现货 | ||
25 mg | ¥ 3,590 | 现货 | ||
50 mg | ¥ 5,180 | 现货 | ||
100 mg | ¥ 7,330 | 现货 | ||
500 mg | ¥ 14,600 | 现货 |
产品描述 | AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux. |
靶点活性 | mGluR5 (human):7.6±1.1 nM, mGluR5 (rat):2.6±0.3 nM |
体外活性 | AZD9272 (10 μM) does not diminish the response to 10 μM ATP in the background GHEK cells. Increasing concentrations of AZD9272 causes a decrease in the potency and the maximal response of DHPG.[1] AZD9272 completely reverses the glutamate-stimulated (EC80=80 μM) phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with IC50 of 26±3 nM (n=21).[1] |
体内活性 |
AZD 9272 (3 μmol/kg; single intravenous) is eliminated from plasma with terminal half-lives between 2 and 6 h. The terminal half-lives following oral dosing are similar to the half-lives following intravenous dosing. The volume of distribution at steady state is intermediate for AZD9272.[1] AZD9272 (2.84 mg/kg) causes greater than 80% and typically more than 99% MTEP-appropriate responding up to 20 hours after dose, with a decline to approximately 20% at 24 hours after dose, yielding a t1/2 of 21.93 hours, and causes no systematic effects on response rates. The first-time point at which AZD9272 causes >90% MTEP-appropriate response is at 30 minutes after the dose.[2] |
分子量 | 284.22 |
分子式 | C14H6F2N4O |
CAS No. | 327056-26-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.8 mg/mL (45.0 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.5184 mL | 17.592 mL | 35.184 mL | 87.96 mL |
5 mM | 0.7037 mL | 3.5184 mL | 7.0368 mL | 17.592 mL | |
10 mM | 0.3518 mL | 1.7592 mL | 3.5184 mL | 8.796 mL | |
20 mM | 0.1759 mL | 0.8796 mL | 1.7592 mL | 4.398 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。
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