Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tebanicline hydrochloride (Ebanicline hydrochloride) 是一种有效的合成烟碱(non-opioid)镇痛药。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 275 | 现货 | ||
2 mg | ¥ 495 | 现货 | ||
5 mg | ¥ 892 | 现货 | ||
10 mg | ¥ 1,360 | 现货 | ||
25 mg | ¥ 2,680 | 现货 | ||
50 mg | ¥ 3,920 | 现货 | ||
100 mg | ¥ 5,690 | 现货 | ||
500 mg | ¥ 11,800 | 现货 |
产品描述 | Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug. |
靶点活性 | nAChR:37 pM(ki) |
体外活性 | Tebanicline is a novel, potent cholinergic nAChR ligand with analgesic properties that shows preferential selectivity for neuronal nAChRs. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM. Functionally, tebanicline is an agonist. At the transfected human α4β2 neuronal nAChR in K177 cells, with increased 86Rb+ efflux as a measure of cation efflux, ABT-594 has an EC50 value of 140 nM with an intrinsic activitycompared with (?)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells, an EC50 of 340 nM; at the F11 dorsal root ganglion cell line, an EC50 of 1220 nM; and via direct measurement of ion currents, an EC50 value of 56,000 nM at the human α7 homo-oligimeric nAChR produced in oocytes[1] |
体内活性 | Tebanicline is a potent antinociceptive agent with full efficacy in models of acute and persistent pain and that these effects are mediated predominately by an action at central neuronal nAChRs[2]. Tebanicline produces significant antinociceptive effects in mice against both acute noxious thermal stimulation. ABT-594 is orally active, but 10-fold less potent by this route than after i.p. administration. The antinociceptive effect of ABT-594 is prevented, but not reversed, by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist[3]. Tebanicline has antinociceptive effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Direct injection of tebanicline into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and destruction of serotonergic neurons in the NRM attenuates the effect of systemic tebanicline[4]. |
别名 | 替巴克兰盐酸盐, ABT-594 hydrochloride, Ebanicline hydrochloride |
分子量 | 235.11 |
分子式 | C9H12Cl2N2O |
CAS No. | 203564-54-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 34 mg/mL (144.61 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.2533 mL | 21.2666 mL | 42.5333 mL | 106.3332 mL |
5 mM | 0.8507 mL | 4.2533 mL | 8.5067 mL | 21.2666 mL | |
10 mM | 0.4253 mL | 2.1267 mL | 4.2533 mL | 10.6333 mL | |
20 mM | 0.2127 mL | 1.0633 mL | 2.1267 mL | 5.3167 mL | |
50 mM | 0.0851 mL | 0.4253 mL | 0.8507 mL | 2.1267 mL | |
100 mM | 0.0425 mL | 0.2127 mL | 0.4253 mL | 1.0633 mL |
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。
Tebanicline hydrochloride 203564-54-9 Neuroscience AChR ABT 594 Hydrochloride 替巴克兰盐酸盐 ABT594 Hydrochloride ABT-594 hydrochloride Ebanicline hydrochloride ABT-594 Hydrochloride Tebanicline Hydrochloride Ebanicline Hydrochloride Inhibitor inhibitor inhibit