Pumosetrag-Hydrochloride-MKC-733-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPumosetrag HydrochlorideCat. No.: HY-19650CAS No.: 194093-42-0Synonyms: MKC-733; DDP-733分式: CHClNOS分量: 339.84作靶点: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C

2、 1 month溶解性数据体外实验 DMSO : 30 mg/mL (88.28 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9426 mL 14.7128 mL 29.4256 mL5 mM 0.5885 mL 2.9426 mL 5.8851 mL10 mM 0.2943 mL 1.4713 mL 2.9426 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Pumosetra

3、g Hydrochloride (MKC-733; DDP-733)种服可的 5-HT3 部分激动剂，开发来治疗肠易激综合征和胃管反流病。IC50 & Target 5-HT3 1体内研究Pumosetrag displays both regional and species specificities. Pumosetrag has a lower efficacy than 5-HT in1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEthe rat jejunum, ileum and distal colon; however, it

4、 has similar efficacy and potency to 5-HT in the ratproximal colon. The activity profile of Pumosetrag is different in the guinea pig intestine where it exhibitsgreater potency and efficacy than 5-HT in all regions. Pumosetrag shows little to no response in the regionsof the mouse intestine. Respons

5、es to Pumosetrag in the rat and guinea pig tissues are inhibited byondansetron, confirming its action on 5-HT(3) receptors 1. Pumosetrag delays liquid gastric emptying inassociation with relaxation of the proximal stomach, stimulates fasting antroduodenal migrating motorcomplex activity and accelera

6、tes small intestinal transit 2.REFERENCES1. 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 PharmacolTher. 2003 Nov 15;18(10):1039-48.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel