Nisoxetine hydrochloride ≥98%
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| 包装规格: | 5mg in glass bottle |
| 产品描述: | 基本信息 产品编号: N11038 产品名称: Nisoxetine hydrochloride CAS: 57754-86-6 储存条件 粉末 -20℃ 四年 分子式: C17H22ClNO2 溶于液体 -80℃ 6个月 分子量: 307.82 -20℃ 1个月 化学名: Benzenepropanamine,gamma-(2-methoxyphenoxy)-N-methyl-,hydrochloride,(+-)- Solubility (25°C): 体外: DMSO Ethanol 'mg/mL Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 3.2487mL 16.2433mL 32.4865mL 5mM 0.6497mL 3.2487mL 6.4973mL 10mM 0.3249mL 1.6243mL 3.2487mL 生物活性 产品描述 一种有效的和选择性的去甲肾上腺素转运蛋白(NET)的抑制剂,Kd值为0.76nM。Nisoxetinehydrochloride是一种抗抑郁药和局部麻药,它可以阻断电压门控性钠通道。 靶点 Kd:0.76nM (NET) 体外研究 Nisoxetine inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1nM.Nisoxetine inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3nM.Nisoxetine inhibits Na+currents with IC50s of 1.6 and 28.6µM at the membrane potential of -70 and -100 mV,respectively. 体内研究 Nisoxetine (0.6-2.2µM;a single intrathecal injection) displays dose-dependent effects on spinal anesthesia in rats.Nisoxetine (2.2µM;a single intrathecal injection) shows 100,100,and 100% of blockades in motor function,proprioception,and with duration of action of about 61,96,and 236 min,respectively. Animal Model: Sprague-Dawley rats(290-340g) Dosage: 0.6,1.2,1.8,2.2µM Administration: A single intrathecal injection Result: With ED50s of 0.82,0.75 and 0.70µM in motor function,proprioception,and nociception respectively. |
| 保存条件: | -20℃ |
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