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Pumosetrag Hydrochloride is an orally available 5-HT3 partial agonist. It is developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.


| Description | Pumosetrag Hydrochloride is an orally available 5-HT3 partial agonist. It is developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease. |
| In vivo | Pumosetrag modulates gastrointestinal activity by delaying liquid gastric emptying through proximal stomach relaxation and enhancing fasting antroduodenal migrating motor complex activity, while also speeding up small intestinal transit. Its effectiveness varies across different sections of the mouse intestine, displaying minimal to no activity. This compound demonstrates regional and species-specific responses, with reduced efficacy compared to 5-HT in the rat's jejunum, ileum, and distal colon, yet showing comparable efficacy and potency in the rat's proximal colon. In contrast, Pumosetrag is more potent and effective than 5-HT across all regions of the guinea pig intestine. Its mechanism, mediated by 5-HT(3) receptors, is confirmed by the inhibitory effect of ondansetron on its actions in rat and guinea pig tissues. |
| Synonyms | MKC-733, DDP-733 |
| Molecular Weight | 339.84 |
| Formula | C15H18ClN3O2S |
| Cas No. | 194093-42-0 |
| Smiles | Cl.O=C(N[C@H]1CN2CCC1CC2)c1c[nH]c2ccsc2c1=O |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (88.28 mM), Sonication and heating are recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.5 mg/mL (4.41 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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