货号:A293957 同义名: 曲司氯胺 / Trospium (chloride);Relaspium
Trospium chloride是一种竞争性拮抗剂,作用于毒蕈碱型胆碱受体,用于治疗膀胱过度活跃的症状。
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产品名称 | AChE ↓ ↑ | AChR ↓ ↑ | mAChR ↓ ↑ | nAChR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Donepezil |
+++
hAChE, IC50: 11.6 nM bAChE, IC50: 8.12 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 | 99% | ||||||||||||||||
Pyridostigmine bromide | ✔ | 99+% | |||||||||||||||||
Rivastigmine |
+
AChR, IC50: 5.5 μM |
98% | |||||||||||||||||
Paroxetine hydrochloride | ✔ | 99% | |||||||||||||||||
Rocuronium Bromide | ✔ | 98% | |||||||||||||||||
Tropicamide |
+++
M4 mAChR, IC50: 8 nM |
98% | |||||||||||||||||
Diphenmanil methylsulfate | ✔ | 99% | |||||||||||||||||
Umeclidinium bromide | ✔ | 95% | |||||||||||||||||
Otilonium bromide | ✔ | 98% | |||||||||||||||||
Flavoxate HCl |
+
mAChR, IC50: 12.2 μM |
99% | |||||||||||||||||
Ipratropium bromide | ✔ | 98% | |||||||||||||||||
Diphenidol HCl | ✔ | 98% | |||||||||||||||||
Darifenacin hydrobromide |
++++
M3 mAChR, pKi: 8.9 |
98% | |||||||||||||||||
Aclidinium Bromide |
++++
M2 mAChR, Ki: 0.1 nM M4 mAChR, Ki: 0.21 nM |
98% | |||||||||||||||||
Oxybutynin chloride | ✔ | 99% | |||||||||||||||||
Pentoxyverine citrate | ✔ | 98% | |||||||||||||||||
Solifenacin | ✔ | 98% | |||||||||||||||||
Catharanthine | ✔ | 98% | |||||||||||||||||
Benzethonium chloride |
+++
α7 nAChRs, IC50: 122 nM α4β2 nAChRs, IC50: 49 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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,2-8°C |
溶解方案 |
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) 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |