Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 794 | 5日内发货 | ||
25 mg | ¥ 6,120 | 6-8周 | ||
50 mg | ¥ 7,950 | 6-8周 | ||
100 mg | ¥ 12,100 | 6-8周 |
产品描述 | A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo. |
靶点活性 | Nav1.8:11 nM |
体外活性 | A-887826 is approximately 3 fold less potent to block Na(v)1.2, approximately 10 fold less potent to block tetrodotoxin-sensitive sodium (TTX-S Na(+)) currents and is >30 fold less potent to block Na(v)1.5 channels. A-887826 potently blocks tetrodotoxin-resistant sodium (TTX-R Na(+)) currents (IC50: 8 nM) from small diameter rat dorsal root ganglion (DRG) neurons in a voltage-dependent fashion. A-887826 effectively suppresses evoked action potential firing when DRG neurons are held at depolarized potentials and reversibly suppresses spontaneous firing in small-diameter DRG neurons from complete Freund's adjuvant inflamed rats. A-887826 (100 nM) shifts the mid-point of voltage-dependent inactivation of TTX-R currents by approximately 4mV without affecting voltage-dependent activation and does not exhibit frequency-dependent inhibition. |
体内活性 | A-887826 (3-30 mg/kg; p.o.; 1-hour pre-treatment) significantly attenuates tactile allodynia in a rat neuropathic pain model. |
动物实验 | Animal Model: Male Spraguee Dawley rats (200-300 g). Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg. Administration: p.o.; 1 hour before testing; fourteen days after L5-L6 spinal nerve ligation |
分子量 | 480.99 |
分子式 | C26H29ClN4O3 |
CAS No. | 1266212-81-0 |
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。
A-887826 1266212-81-0 Others A 887826 A887826 Inhibitor inhibitor inhibit