Mosapride citrate
Based on 6 publication(s) in Google Scholar
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.
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- Pureté : 99.82%
- CAS No.: 112885-42-4
- Formule: C27H33ClFN3O10
- Masse moléculaire:614.02
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Mosapride5HT4 Agonist
Publications Citing Use of MedChemExpress (MCE) Mosapride citrate
MoreVoir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
Description
IC50 & Target
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5-HT4 Receptor |
In Vitro
Mosapride citrate (1-100 nM) significantly increases the average amplitude of proximal and distal colon contraction, and shortens the transport time of proximal and distal colon in guinea-pig[3].
Mosapride citrate (869 ng/mL, 48 h) increases the induction ability of Cytochrome P450 (CYP1A2, 2B6 and 3A4) in human hepatocytes (HMC424, 478 and 493)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Mosapride citrate (0.5 mg/kg, p.o) can relieve NSAIDS induced ulcer by activating 5-HT4 receptor in rats[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSAID-induced experimental ulcer model[6]
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Dosage:0.25, 0.5 , 0.75 mg/kg
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Administration:p.o
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Result:Inhibited the mucosal damage.
Chemical Information
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CAS No. 112885-42-4
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Appearance Solid
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Masse moléculaire 614.02
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Formule C27H33ClFN3O10
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Color White to off-white
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SMILES
O=C(NCC1CN(CC2=CC=C(F)C=C2)CCO1)C3=CC(Cl)=C(N)C=C3OCC.O=C(CC(C(O)=O)(O)CC(O)=O)O
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Synonyms
TAK-370 citrate; AS-4370 citrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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J Ethnopharmacol
Yiqi Kaimi prescription regulates protein phosphorylation to promote intestinal motility in slow transit constipation. [Abstract]2024 Jul 15:329:118118. PMID: 38614261 -
Chin J Integr Med
Zhizhu Decoction Alleviates Intestinal Barrier Damage via Regulating SIRT1/FoxO1 Signaling Pathway in Slow Transit Constipation Model Mice. [Abstract]2023 Sep;29(9):809-817. PMID: 36044116 -
Dig Dis Sci
Kaempferol Ameliorates Functional Constipation in Mice by Regulating Autophagy of Interstitial Cells of Cajal via the p53/AMPK/mTOR Axis. [Abstract]2025 Nov 15. PMID: 41240265 -
J Appl Microbiol
Houpo Paiqi Mixture Promotes Intestinal Motility in Constipated Rats by Modulating Gut Microbiota and Activating 5-HT-cAMP-PKA Signal Pathway. [Abstract]2023 Aug 1;134(8):lxad153. PMID: 37481692 -
Drug Metab Pharmacokinet
2020 Feb;35(1):102-110. PMID: 31732429 -
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (162.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Tack J, et al. Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders. Aliment Pharmacol Ther. 2012 Apr;35(7):745-67. [Content Brief]
[2]. Curran MP, et al. Mosapride in gastrointestinal disorders. Drugs. 2008;68(7):981-91. [Content Brief]
[3]. Kim HS, et al. The effect of mosapride citrate on proximal and distal colonic motor function in the guinea-pig in vitro. Neurogastroenterol Motil. 2008 Feb;20(2):169-76. [Content Brief]
[4]. Kim YH, et al. Measurement of Human Cytochrome P450 Enzyme Induction Based on Mesalazine and Mosapride Citrate Treatments Using a Luminescent Assay. Biomol Ther (Seoul). 2015 Sep;23(5):486-92. [Content Brief]
[5]. Uchida M, et al. Dual role of mosapride citrate hydrate on the gastric emptying evaluated by the breath test in conscious rats. J Pharmacol Sci. 2013;121(4):282-7. [Content Brief]
[6]. Fujisawa M, et al. The 5-HT4 receptor agonist mosapride attenuates NSAID-induced gastric mucosal damage. J Gastroenterol. 2010 Feb;45(2):179-86. [Content Brief]
[7]. Sung KW, et al. Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2013 Oct;386(10):905-16. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6286 mL | 8.1431 mL | 16.2861 mL | 40.7153 mL |
| 5 mM | 0.3257 mL | 1.6286 mL | 3.2572 mL | 8.1431 mL | |
| 10 mM | 0.1629 mL | 0.8143 mL | 1.6286 mL | 4.0715 mL | |
| 15 mM | 0.1086 mL | 0.5429 mL | 1.0857 mL | 2.7144 mL | |
| 20 mM | 0.0814 mL | 0.4072 mL | 0.8143 mL | 2.0358 mL | |
| 25 mM | 0.0651 mL | 0.3257 mL | 0.6514 mL | 1.6286 mL | |
| 30 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3572 mL | |
| 40 mM | 0.0407 mL | 0.2036 mL | 0.4072 mL | 1.0179 mL | |
| 50 mM | 0.0326 mL | 0.1629 mL | 0.3257 mL | 0.8143 mL | |
| 60 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 mL | |
| 80 mM | 0.0204 mL | 0.1018 mL | 0.2036 mL | 0.5089 mL | |
| 100 mM | 0.0163 mL | 0.0814 mL | 0.1629 mL | 0.4072 mL |
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