Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CPPHA 是一种谷氨酸受体 mGluR5 和 mGluR1的 正向变构调制剂,常用于开发用于中枢神经系统疾病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
5 mg | ¥ 567 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 1,950 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 625 | 现货 |
产品描述 | CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases. |
体外活性 | CPPHA增强了亚阈浓度的3,5-二羟基苯甘氨酸(DHPG)对细胞外信号调节蛋白激酶(ERK)和cAMP响应元件结合蛋白(CREB)活性的影响,以及在皮层和海马切片中的N-甲基-D-天门冬氨酸(NMDA)受体亚单位NR1的磷酸化[1]。CPPHA将荧光Ca(2+)测定中对谷氨酸的阈反应增强了7至8倍(EC50s:400至800nM),并在10微摩尔浓度下将mGluR5激动剂对谷氨酸、鹿蕨酸和DHPG的浓度反应曲线向左移动了4至7倍。10微摩尔的CPPHA增强了海马切片中由DHPG诱导的NMDA受体电流,尽管它本身对这些电流没有影响。同样,10微摩尔的CPPHA也增强了大鼠下丘脑神经元DHPG诱发的mGluR5介导的去极化[2]。CPPHA提升了基础mGluR5介导的ERK1/2磷酸化水平,并增强了低浓度激动剂的效应。相比之下,CPPHA显著降低了高浓度激动剂诱导的ERK1/2磷酸化[3]。 |
细胞实验 | CPPHA potentiated the response to a subthreshold concentration of 3,5-dihydroxy-phenylglycine (DHPG) on extracellular signal-regulated protein kinase (ERK) and cyclic-AMP responsive element-binding protein (CREB) activity, as well as N-methyl d-aspartate (NMDA) receptor subunit NR1 phosphorylation in cortical and hippocampal slices [1]. CPPHA potentiated threshold responses to glutamate in fluorometric Ca(2+) assays 7- to 8-fold (EC50s: 400 to 800 nM), and at 10 μM shifted mGluR5 agonist concentration-response curves to glutamate, quisqualate, and DHPG 4- to 7-fold to the left. CPPHA (10 μM) potentiated NMDA receptor currents in hippocampal slices induced by threshold levels of DHPG, whereas having no effect on these currents by itself. Similarly, 10 μM CPPHA also potentiated mGluR5-mediated DHPG-induced depolarization of rat subthalamic nucleus neurons [2]. CPPHA induced an increase in basal mGluR5-mediated ERK1/2 phosphorylation and potentiated the effect of low concentrations of agonists. In contrast, CPPHA significantly decreased ERK1/2 phosphorylation induced by high concentrations of agonists [3]. |
分子量 | 406.82 |
分子式 | C22H15ClN2O4 |
CAS No. | 693288-97-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.0 mg/mL (221.2 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4581 mL | 12.2904 mL | 24.5809 mL | 61.4522 mL |
5 mM | 0.4916 mL | 2.4581 mL | 4.9162 mL | 12.2904 mL | |
10 mM | 0.2458 mL | 1.229 mL | 2.4581 mL | 6.1452 mL | |
20 mM | 0.1229 mL | 0.6145 mL | 1.229 mL | 3.0726 mL | |
50 mM | 0.0492 mL | 0.2458 mL | 0.4916 mL | 1.229 mL | |
100 mM | 0.0246 mL | 0.1229 mL | 0.2458 mL | 0.6145 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。
CPPHA 693288-97-0 Neuroscience GluR Inhibitor inhibitor inhibit