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Pumosetrag Hydrochloride(MKC-733)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pumosetrag Hydrochloride(MKC-733)图片
CAS NO:194093-42-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Pumoserag Hydrochloride (MKC-733) (MKC-733; DDP-733) 是一种口服 5-HT3 部分激动剂,用于治疗肠易激综合征和胃食管反流病。
Cas No.194093-42-0
别名7-氧代-N-[3(R)-奎宁环基]-4,7-二氢噻吩并[3,2-B]吡啶-6-甲酰胺盐酸盐,MKC-733; DDP-733
Canonical SMILESO=C(C1=CNC(C=CS2)=C2C1=O)N[C@H]3CN4CCC3CC4.[H]Cl
分子式C15H18ClN3O2S
分子量339.84
溶解度DMSO : 30 mg/mL (88.28 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.

Pumosetrag displays both regional and species specificities. Pumosetrag has a lower efficacy than 5-HT in the rat jejunum, ileum and distal colon; however, it has similar efficacy and potency to 5-HT in the rat proximal colon. The activity profile of Pumosetrag is different in the guinea pig intestine where it exhibits greater potency and efficacy than 5-HT in all regions. Pumosetrag shows little to no response in the regions of the mouse intestine. Responses to Pumosetrag in the rat and guinea pig tissues are inhibited by ondansetron, confirming its action on 5-HT(3) receptors[1]. Pumosetrag delays liquid gastric emptying in association with relaxation of the proximal stomach, stimulates fasting antroduodenal migrating motor complex activity and accelerates small intestinal transit[2].

[1]. Chetty N, et al. Effects of the novel 5-HT3 agonist MKC-733 on the rat, mouse and guinea pig digestive tract. Pharmacology. 2008;81(2):104-9. Epub 2007 Oct 19. [2]. Coleman NS, et al. Effect of a novel 5-HT3 receptor agonist MKC-733 on upper gastrointestinal motility in humans. Aliment Pharmacol Ther. 2003 Nov 15;18(10):1039-48.