产品说明
生化/生理作用
ORG 25543 is a brain-penetrant (free brain/plasma ratio = 0.53; 35 min post 2 or 20 mg/kg i.v. in mice), high-affinity, potent and selective glycine transporter 2 (GlyT-2; GlyT2) inhibitor (human & mouse pIC50 = 7.9/ GlyT2 vs <4/GlyT1) with great selectivity over a panel of 56 receptor and channel proteins. ORG 25543 is more potent and selective than the brain-impermeable ALX-1393 (GlyT2/GlyT1 pIC50 = 7.1/5.4) and exhibits high in vivo efficacy in a murine diabetic neuropathic pain model (ED50 = 0.07-0.16 mg/kg i.v.; Emin = 0.01 mg/kg). ORG 25543 is practically irreversible due to its tight-binding nature, suboptimal dosage should be applied in vivo to allow low target occupancy only and minimize acute toxicity.
基本信息
| 经验(实验)分子式 | C24H32N2O4·HCl |
| 分子量 | 448.98 |
| MDL编号 | MFCD23701926 |
产品性质
| 测定 | ≥95% (HPLC) |
| 形式 | powder |
| 储存条件 | desiccated |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | room temp |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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