Pumosetrag Hydrochloride|194093-42-0|(MKC-733; DDP-733)-陌孚医药/Medlife

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Pumosetrag Hydrochloride (Synonyms: MKC-733; DDP-733)

目录号: PL04916 纯度: ≥99%

CAS No. :194093-42-0

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中文名称	Pumosetrag Hydrochloride
中文别名	Pumosetrag 盐酸盐;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;Pumosetrag 盐酸盐; 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;PUMOSETRAG 盐酸盐;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
英文名称	Pumosetrag Hydrochloride
英文别名	Pumosetrag hydrochloride;7-Oxo-N-[3(R)-quinuclidinyl]-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamide hydrochloride;MKC-733;N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-7-oxo-4H-thieno[3,2-b]pyridine-6-carboxamide,hydrochloride;(R)-N-(1-azabicy;(R)-N-(1-azabicyclo[2.2.2]oct-3-yl)-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide hydrochloride;(R)-N-(3-quinuclidinyl)-7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamide hydrochloride;(R)-N-(3-Quinuclidinyl)-7-oxo-dihydrothieno(3,2b)pyridine-6-carboxamide hydrochloride;(R)-N-1-azabicyclo[2.2.2]oct-3-yl-4,7-dihydro-7-oxothieno[3,2-b]pyridine-6-carboxamide monohydrochloride;AC1L4BP9;DDP-733;DPP 733;SureCN1497905;DDP733;N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide hydrochloride;Pumosetrag;PuMosetrag hydrochloride MKC-733;N-[(8R)-1-azabicyclo[2.2.2]oct-8-yl]-2-oxo-9-thia-5-azabicyclo[4.3.0]n ona-3,7,10-triene-3-carboxamide hydrochloride
Cas No.	194093-42-0
分子式	C₁₅H₁₇N₃O₂S^.HCl
分子量	339.84
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

Pumosetrag Hydrochloride (MKC-733; DDP-733) 是一种口服可用的 5-HT3 部分激动剂，可用于肠易激综合征和胃食管反流病的研究。

生物活性

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.

性状

Solid

IC50 & Target[1][2]

5-HT3 Receptor

体内研究(In Vivo)

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. 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. has not independently confirmed the acc

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]. 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.

溶解度数据	In Vitro: DMSO : 12 mg/mL (35.31 mM; Need ultrasonic)H₂O : 2.94 mg/mL (8.65 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

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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