Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XAP044 是高效的选择性mGlu7拮抗剂。代谢型谷氨酸受体亚型 7 是哺乳动物 CNS 中神经传递的重要突触前调节剂。它在啮齿动物行为测试中表现出较好的大脑暴露、广谱抗应激、抗抑郁以及抗焦虑作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 479 | 现货 | ||
2 mg | ¥ 697 | 现货 | ||
5 mg | ¥ 997 | 现货 | ||
10 mg | ¥ 1,890 | 现货 | ||
25 mg | ¥ 3,390 | 现货 | ||
50 mg | ¥ 4,930 | 现货 | ||
100 mg | ¥ 6,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,220 | 现货 |
产品描述 | XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1]. |
体外活性 | Previous study showed that in contrast to all previous mGlu7-selective drugs, XAP044 did not act through the seven-transmembrane region but rather via a binding pocket localized in mGlu7's extracellular Venus flytrap domain, a region identified for orthosteric agonist binding, which was suggested by the chimeric receptor studies in recombinant cell line assays [1]. |
体内活性 | In rodent behavioral paradigms, XAP044 demonstrated good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy. In addition, XAP044 could reduce freezing during acquisition of Pavlovian fear and innate anxiety, which was consistent with the phenotypes of mGlu7-deficient mice. Moreover, XAP044 was able to inhibit lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm. It was alos found that there was no effect of XAP044 on LTP of mGlu7-deficient mice, suggesting that such pharmacological effect was mGlu7-dependent [1]. |
分子量 | 380.13 |
分子式 | C15H9IO4 |
CAS No. | 196928-50-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (157.84 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6307 mL | 13.1534 mL | 26.3068 mL | 65.767 mL |
5 mM | 0.5261 mL | 2.6307 mL | 5.2614 mL | 13.1534 mL | |
10 mM | 0.2631 mL | 1.3153 mL | 2.6307 mL | 6.5767 mL | |
20 mM | 0.1315 mL | 0.6577 mL | 1.3153 mL | 3.2883 mL | |
50 mM | 0.0526 mL | 0.2631 mL | 0.5261 mL | 1.3153 mL | |
100 mM | 0.0263 mL | 0.1315 mL | 0.2631 mL | 0.6577 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。
XAP044 196928-50-4 Neuroscience GluR mGlu7 neurotransmission brain exposure CNS XAP-044 inhibit mGluR antidepressant Metabotropic glutamate receptors wide spectrum XAP 044 anti-stress Inhibitor anxiolytic-like inhibitor