MKC-733

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性、口服活性 5-HT3 受体激动剂，对犬肠道平滑肌 5-HT3 受体具有高亲和力。

A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors; dose dependently stimulates contraction and basal electrolyte secretion in the isolated guinea pig colon, effects that are antagonized by the selective 5-HT3 antagonist ondansetron, also accelerates gastric emptying in some animal models.Irritable Bowel Syndrome Phase 2 Discontinued.

——

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.

MKC733 | Pumosetrag | DDP 733

GPCR/G Protein

5-HT Receptor

5-HT Receptor

Other Indications

Irritable Bowel Syndrome

194093-42-0

39.838

C15H18ClN3O2S

>98% (HPLC)

DMSO : 30 mg/mL 88.28 mM

O=C(C1=CNC(C=CS2)=C2C1=O)N[C@H]3CN4CCC3CC4.[H]Cl

Thieno[3,2-b]pyridine-6-carboxamide, N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4,7-dihydro-7-oxo-, monohydrochloride (9CI)

(-20℃)

With Ice Pack

≥ 2 years