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  • 化合物 Tebanicline dihydrochloride|T60474|TargetMol

化合物 Tebanicline dihydrochloride|T60474|TargetMol

Tebanicline dihydrochloride
209326-19-2
491 2mg 起订
822 5mg 起订
上海 更新日期:2025-11-17

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 Tebanicline dihydrochloride
英文名称:
Tebanicline dihydrochloride
CAS号:
209326-19-2
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别:
抑制剂
货号:
T60474

Product Introduction

Bioactivity

名称Tebanicline dihydrochloride
描述Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with effective orally analgesic activity. Tebanicline dihydrochloride inhibits the cytisine binding to α4β2 neuronal nAChRs with a Ki of 37 pM [1].
体外活性Tebanicline is a novel and effective cholinergic nAChR ligand with analgesic properties and preferential selectivity for neuronal nAChRs. Tebanicline inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM. Tebanicline is functionally an agonist. At the transfected human alpha 4 beta 2 neuronal nAChR (K177 cells), with increased 86Rb+ efflux as a measure of cation efflux, Tebanicline had an EC50 value of 140 nM with an intrinsic activity (IA) compared with (-)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells (sympathetic ganglion-like), an EC50 of 340 nM (IA = 126%); at the F11 dorsal root ganglion cell line (sensory ganglion-like), an EC50 of 1220 nM (IA = 71%); and via direct measurement of ion currents, an EC50 value of 56,000 nM (IA = 83%) at the human alpha 7 homooligimeric nAChR produced in oocytes.
体内活性Tebanicline is a potent analgesic with full efficacy in models of acute and persistent pain and these effects are primarily mediated by an action at central neuronal nAChRs [2]. Tebanicline produces significant analgesic effects in mice in response to acute noxious thermal stimulation. ABT-594 is orally active, but 10-fold less potent by this route than after intraperitoneal injection. The analgesic effect of ABT-594 is blocked, but not reversed, by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist [3]. Tebanicline has analgesic effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Injection of tebanicline directly into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and disruption of serotonergic neurons in the NRM attenuates the effect of systemic tebanicline [4].
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
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Tebanicline dihydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (13年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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