Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and has good blood-brain barrier permeability.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 660 | 5日内发货 | ||
25 mg | ¥ 4,150 | 6-8周 | ||
50 mg | ¥ 5,390 | 6-8周 | ||
100 mg | ¥ 9,360 | 6-8周 |
产品描述 | GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and has good blood-brain barrier permeability. |
靶点活性 | AMPA receptor:11 μM , Kainate receptor:7.5 μM |
体外活性 | GYKI 52466 also suppresses non-NMDA receptor-mediated spontaneous synaptic currents via a postsynaptic action.In kinetic experiments with kainate as the agonist, the GYKI 52466 binding and unbinding rates were 1.6 x 105 M-1 s-1 and 3.2 s-1, respectively. |
体内活性 | GYKI 52466 provides potent anticonvulsant protection against AMPA-induced seizures in Swiss mice. Maximal anticonvulsant protection is observed 5-15 min after the i.p. administration of GYKI 52466 in DBA/2 mice. The ED50 values for the protection against AMPA-induced seizures by GYKI 52466 (15 min, i.p.) is 18.5 (11.5-29.5) μmol/kg.GYKI 52466 (1.76-13.2 mg/kg;?male and female DBA/2 mice;?intraperitoneal injection) treatment provides potent anticonvulsant protection against sound-induced seizures in seizure-susceptible DBA/2 mice.?The ED50 value at 15 min for the protection against sound-induced seizures in DBA/2 mice is 13.7 (11.5-16.5) μmol/kg (GYKI 52466, i.p.). |
分子量 | 366.24 |
分子式 | C17H17Cl2N3O2 |
CAS No. | 2319722-40-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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