购物车
- 全部删除
- 您的购物车当前为空
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 785 | 现货 |
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 | Kainate receptor:7.5 μM , AMPA receptor:11 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 |
存储 | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.