Cimetropium Bromide (Synonyms: 西托溴铵; DA-3177)
目录号: PL06891 纯度: ≥96%
CAS No. :51598-60-8
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中文名称
Cimetropium Bromide
中文别名
西托溴铵;溴化N-(环丙基甲基)东莨菪碱
英文名称
Cimetropium Bromide
英文别名
(7(S)-(1alpha,2beta,4beta,5alpha,7beta))-9-(Cyclopropylmethyl)-7-(3-hydroxy-1-oxo-2-phenylpropoxy)-9-methyl-3-oxa-9-azoniatricyclo(3.3.1.0(sup 2,4))nonane bromide;3-Oxa-9-azoniatricyclo[3.3.1.02,4]nonane, 9-(cyclopropylmethyl)-7-[(2S)-3-hydroxy-1-oxo-2-phenylpropoxy]-9-methyl-, bromide (1:1), (1α,2β,4β,5α,7β)-;CIMETRONIN BROMIDE;da3177;N-Cyclopropvlmethylscopolamine bromide
Cas No.
51598-60-8
分子式
C21H28BrNO4
分子量
438.35
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Cimetropium Bromide (DA-3177) 是一种毒蕈碱受体拮抗剂,用于长期研究肠易激综合征。
生物活性
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
性状
Solid
IC50 & Target[1][2]
mAChR
体外研究(In Vitro)
Cimetropium Bromide behaves as a competitive antagonist of muscarinic-mediated contractions in isolated colonic preparations from both species, with affinity values (pA2) ranging between 7.41 and 7.82. Cimetropium has potent antimuscarinic effect in inhibition of contraction of longitudinal muscle preparations. In the superfusion experiments of the preparation which has been preloaded with labelled choline, Cimetropium decreases the labelled ACh release induced by electrical field stimulation under the muscarinic autoinhibition blocked-condition. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
When administered intravenously to conscious dogs provided with a colonic Thiry fistula, Cimetropium is a potent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. Cimetropium Bromide (10-100 μg/kg) counteracts colonic motor response to neostigmine administration with an ID 50 of 27.9 μg/kg; both tonic and phasic components of contractile response are affected. In a comparable range of doses (3-100μg/kg), the drug inhibits motor activity elicited by intraluminal distension. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Identification of orally administered cimetropium bromide in the colon of the rat and its possible local spasmolytic effect.
[2]. Saitoh N, et al. Characterization of antimuscarinic effect of cimetropium bromide in guinea pig ileum. J Smooth Muscle Res. 1997 Feb;33(1):1-9.
溶解度数据
In Vitro: H2O : 50 mg/mL (114.06 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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