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曲司氯铵 /Trospium chloride {[allProObj[0].p_purity_real_show]}

货号:A293957 同义名: 曲司氯胺 / Trospium (chloride);Relaspium

Trospium chloride is a competitive antagonist at muscarinic cholinergic receptors, used to treat symptoms of an overactive bladder.

Trospium chloride 化学结构 CAS号:10405-02-4
Trospium chloride 化学结构
CAS号:10405-02-4
Trospium chloride 3D分子结构
CAS号:10405-02-4
Trospium chloride 化学结构 CAS号:10405-02-4
Trospium chloride 3D分子结构 CAS号:10405-02-4
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Trospium chloride 纯度/质量文件 产品仅供科研

货号:A293957 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

98%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 98+%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 98%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine hydrochloride 97%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 98%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

98%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Trospium chloride 生物活性

靶点
  • AChR

描述 Trospium Chloride is antagonist of acetylcholine muscarinic receptors and the cornerstone of pharmacotherapy for the symptoms of overactive bladder (OAB). Trospium chloride, dosed 20 mg twice daily, is significantly superior to placebo in improving cystometric parameters, reducing urinary frequency, reducing incontinence episodes, and increasing urine volume per micturition[3]. Moreover, trospium chloride (1 mg/kg, intravenously) permeation across the BBB (blood-brain barrier ) is not increased in ageing perse, and therefore, the occurrence of adverse CNS (central nervous system) drug effects is also not expected to increase with ageing[4].

Trospium chloride 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02386072 - Completed - -
NCT00547378 Urinary Incontinence, Urgency-... 展开 >>frequency Overactive Bladder 收起 << Phase 4 Completed - -
NCT01499069 Overactive Bladder Not Applicable Unknown December 2015 Korea, Republic of ... 展开 >> Samsung Medical Center Recruiting Seoul, Korea, Republic of, 135-710 Contact: Kyu-Sung Lee, Ph.D    82-2-3410-3554    ksleedr@skku.edu    Contact: Bong-Hee Lim, BA    82-2-3410-3743    bonghee.lim@sbri.co.kr    Sub-Investigator: Deok Hyun Han, PhD          Sub-Investigator: Young-Suk Lee, PhD          Sub-Investigator: Ha Na Lee, PhD 收起 <<

Trospium chloride 参考文献

[1]Staskin DR. Trospium chloride: Distinct among other anticholinergic agents available for the treatment of overactive bladder. Urol Clin North Am. 2006 Nov;33(4):465-73, viii.

[2]Doroshyenko O, Jetter A, et al. Clinical pharmacokinetics of trospium chloride. Clin Pharmacokinet. 2005;44(7):701-20.

[3]Guay DR. Trospium chloride: an update on a quaternary anticholinergic for treatment of urge urinary incontinence. Ther Clin Risk Manag. 2005 Jun;1(2):157-67. doi: 10.2147/tcrm.1.2.157.62912. PMID: 18360555; PMCID: PMC1661617.

[4]Kranz J, Petzinger E, Geyer J. Brain penetration of the OAB drug trospium chloride is not increased in aged mice. World J Urol. 2013 Feb;31(1):219-24. doi: 10.1007/s00345-011-0803-z. Epub 2011 Nov 27. PMID: 22120415; PMCID: PMC3557395.

Trospium chloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.68mL

2.34mL

1.17mL

23.37mL

4.67mL

2.34mL

Trospium chloride 技术信息

CAS号10405-02-4
分子式C25H30ClNO3
分子量 427.964
别名 曲司氯胺 ;Trospium (chloride);Relaspium
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 35 mg/mL(81.78 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(233.66 mM)

动物实验配方
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