| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Mosapride citrate dihydrate primarily targets the 5-HT4 receptor, acting as an agonist. By activating 5-HT4 receptors on enteric neurons, it stimulates the release of acetylcholine, which enhances gastrointestinal motility. Mosapride also has weak 5-HT3 receptor antagonist activity. It accelerates gastric emptying and improves gastrointestinal transit.
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| ln Vitro |
Mosapride (0.3-30 μM) has concentration-dependent inhibitory action against Kv4.3, with an IC50 of 15.2 μM. Moreover, at subthreshold potentials, moclopride quickens the closed state inactivation and suppresses the open state of Kv4.3 current during depolarization [1].
In vitro, Mosapride citrate dihydrate activates 5-HT4 receptors, increasing cAMP levels in cells expressing these receptors. It stimulates acetylcholine release from enteric neurons. The compound is soluble in aqueous solutions and can be quantified by HPLC or LC-MS. |
| ln Vivo |
It is possible that mosapride preferentially stimulates upper gastrointestinal motility because it dose-dependently increases antral motility activity in awake dogs when administered intravenously at 0.3–3 mg/kg [2].
In vivo, Mosapride citrate dihydrate accelerates gastric emptying and improves gastrointestinal motility in animal models and humans. It is orally active and well-tolerated. The compound is metabolized in the liver and excreted in urine. It is effective in treating functional dyspepsia and gastroesophageal reflux disease. |
| Enzyme Assay |
For 5-HT4 receptor binding assays, membrane fractions from cells expressing 5-HT4 receptors are incubated with [3H]GR113808 in the presence of Mosapride citrate dihydrate at varying concentrations. Reactions are performed in buffer containing 50 mM Tris-HCl (pH 7.4), 5 mM MgCl2, and 1 mM EDTA at 25°C for 60-120 minutes.
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| Cell Assay |
For functional assays, cells expressing 5-HT4 receptors are treated with Mosapride citrate dihydrate, and cAMP accumulation is measured by ELISA. For gastrointestinal motility assays, isolated ileum or colon segments are mounted in organ baths and stimulated electrically, and contraction amplitude is measured.
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| Animal Protocol |
Animal/Disease Models: Beagle dog [2]
Doses: 0.3-3 mg/kg Route of Administration: intravenous (iv) (iv)injection; 0.3-3 mg/kg Experimental Results: Gastric antral motor activity in awake dogs increased in a dose-dependent manner. For in vivo studies, rats or dogs are administered Mosapride citrate dihydrate orally at doses ranging from 0.1-10 mg/kg. Gastric emptying and gastrointestinal transit are measured using charcoal meal or bead expulsion tests. For pharmacokinetic studies, plasma levels of Mosapride are quantified by LC-MS/MS. |
| References |
[1]. Sung KW, et al. Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn-Schmiedeberg's archives of pharmacology. 2013;386(10):905-16.
[2]. Mine Y, et al. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. The Journal of pharmacology and experimental therapeutics. 1997;283(3):1000-8. |
| Additional Infomation |
Mosapride citrate dihydrate is a hydrate.
See also: Mosapride citrate (note moved to). |
| Molecular Formula |
C26H33CLFN3O6
|
|---|---|
| Molecular Weight |
538.00800
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| Exact Mass |
537.204
|
| CAS # |
636582-62-2
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| Related CAS # |
Mosapride citrate;112885-42-4;Mosapride;112885-41-3
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| PubChem CID |
6918047
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| Appearance |
White to off-white solid powder
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| Melting Point |
112-114°C
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| LogP |
4.624
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| tPSA |
134.68
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
44
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| Complexity |
749
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCOC1=CC(N)=C(Cl)C=C1C(NCC2CN(CC3=CC=C(F)C=C3)CCO2)=O.O=C(O)CC(C(O)=O)(O)CC(O)=O.O.O
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| InChi Key |
KVKIQHMTGSGTFO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25ClFN3O3.C6H8O7.2H2O/c1-2-28-20-10-19(24)18(22)9-17(20)21(27)25-11-16-13-26(7-8-29-16)12-14-3-5-15(23)6-4-14;7-3(8)1-6(13,5(11)12)2-4(9)10;;/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);2*1H2
|
| Chemical Name |
4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide;2-hydroxypropane-1,2,3-tricarboxylic acid;dihydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8587 mL | 9.2935 mL | 18.5870 mL | |
| 5 mM | 0.3717 mL | 1.8587 mL | 3.7174 mL | |
| 10 mM | 0.1859 mL | 0.9294 mL | 1.8587 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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