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Tebanicline hydrochloride

Tebanicline hydrochloride

产品编号 T3720   CAS 203564-54-9
别名: 替巴克兰盐酸盐, ABT-594 hydrochloride, Ebanicline hydrochloride

Tebanicline hydrochloride (Ebanicline hydrochloride) 是一种有效的合成烟碱(non-opioid)镇痛药。

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Tebanicline hydrochloride Chemical Structure
Tebanicline hydrochloride, CAS 203564-54-9
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
其他形式的 Tebanicline hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Tebanicline hydrochloride (T3720)
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纯度: 98.71%
纯度: 95%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 34 mg/mL (144.61 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Donnelly-Roberts DL, et al. ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization.J Pharmacol Exp Ther. 1998 May;285(2):777-86. 2. Bannon AW, et al. ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization. J Pharmacol Exp Ther. 1998 May;285(2):787-94. 3. Decker MW, et al. Antinociceptive effects of the novel neuronal nicotinic acetylcholine receptor agonist, ABT-594, in mice. Eur J Pharmacol. 1998 Apr 3;346(1):23-33. 4. Decker MW, et al. The role of neuronal nicotinic acetylcholine receptors in antinociception: effects of ABT-594. J Physiol Paris. 1998 Jun-Aug;92(3-4):221-4.
Asimilobine Oxotremorine M iodide Dimethindene VU0467154 ASM-024 Nitrocaramiphen hydrochloride Myosmine Mebhydrolin napadisylate

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 药物功能重定位化合物库 已知活性化合物库 神经信号分子库 抗阿尔茨海默症化合物库 共价抑制剂库 临床期小分子药物库 NO PAINS 化合物库 经典已知活性库

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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。

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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。

Keywords

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

 

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