| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
\(5-HT_4\) receptor
\(5-HT_3\) receptor (antagonist) [1] |
|---|---|
| ln Vitro |
The average length of the proximal and distal constrictions in the guinea pig water body is dramatically increased by mosaicide citrate (1–100 nM), which also affects the proximal and distal water transit durations [3]. Human liver cells (HMC424, 478, and 493) have increased cytochrome P450 (CYP1A2, 2B6, and 3A4) sensing capability in response to mosapride citrate (869 ng/mL, 48 h) [4].
In the rat esophageal tunica muscularis mucosae, Mosapride exhibits 80–90% of the intrinsic activity of 5-HT, mediating relaxation [1] In the guinea pig distal colon, it has 80–100% of the intrinsic activity of 5-HT, mediating contractile responses [1] In the guinea pig ileum, it only shows 50–60% of the intrinsic activity of 5-HT [1] It has little effect on the rapid component of the delayed rectifying \(K^+\) channels in isolated rabbit Purkinje fibres and ventricular muscle [1] It shows no significant activity on hERG channels in hERG-transfected cells [1] |
| ln Vivo |
In a dose-dependent manner, mosapride citrate (0.3–3 mg/kg or 30 mg/kg dam) facilitates port emptying. A dosage of 30 mg/kg was found to cause significant port emptying [5]. By initiating 5-HT4 absorption in the channel, mosapride citrate (0.25, 0.5, 0.75 mg/kg channel) can mitigate the state brought on by non-steroidal anti-inflammatory drugs [6].
In dogs, Mosapride stimulates gastrointestinal motility [1] In healthy male volunteers, a single oral dose of 10 mg Mosapride does not cause significant changes in pulse, heart rate, QT interval, or ECG parameters [1] In healthy volunteers, co-administration of Mosapride (15 mg/day) with erythromycin for 14 days does not result in ECG changes [1] In patients with diabetic autonomic neuropathy, it enhances gastric motility [1] In asymptomatic volunteers, it affects esophageal motility and bolus transit [1] |
| Cell Assay |
hERG channel activity assay: Culture cells transfected with hERG gene, expose to Mosapride, and detect changes in hERG potassium currents using electrophysiological methods to evaluate the effect on the channel [1]
Gastrointestinal smooth muscle cell/tissue assay: Isolate smooth muscle tissues from rat esophagus, guinea pig distal colon, and guinea pig ileum, incubate with Mosapride, and measure the contractile or relaxant responses of the tissues to assess the intrinsic activity relative to 5-HT [1] Delayed rectifying potassium channel assay: Isolate rabbit Purkinje fibres and ventricular muscle tissues, treat with Mosapride, and record the effect on the rapid component of the delayed rectifying \(K^+\) channels using electrophysiological techniques [1] |
| Animal Protocol |
Animal/Disease Models: NSAID-induced experimental ulcer model
Doses: 0.25, 0.5, 0.75 mg/kg Route of Administration: Oral Experimental Results:Inhibits mucosal damage. Dog gastrointestinal motility assay: Administer Mosapride to dogs via oral route, observe and measure gastrointestinal peristalsis parameters (such as intestinal transit time, motility frequency) to evaluate the prokinetic effect [1] Rat esophageal/colon smooth muscle tissue preparation: Euthanize rats, isolate the esophageal tunica muscularis mucosae and colon smooth muscle tissues, prepare tissue strips, and use them for in vitro contractile/relaxant response experiments [1] Guinea pig ileum/colon tissue preparation: Euthanize guinea pigs, isolate the distal colon and ileum tissues, prepare tissue segments, and use them for in vitro pharmacological activity detection [1] |
| ADME/Pharmacokinetics |
Oral bioavailability: 8% in dogs and 14% in monkeys [1]
Peak plasma time (tmax): 0.5–1.0 hours in humans after oral administration [1] Metabolism: First-pass metabolism in the liver, with M1 as the main metabolite; metabolized by CYP3A4 [1] Excretion: Excreted in urine and feces [1] |
| Toxicity/Toxicokinetics |
No significant cardiovascular toxicity; QT interval prolongation was not observed in healthy volunteers and patients [1]
No electrocardiographic abnormalities were observed when used in combination with erythromycin [1] A case report described a 68-year-old male patient with sick sinus syndrome who developed QTc interval prolongation after treatment with mosapride in combination with flecainide, which may be related to underlying disease and concomitant medication [1] |
| References | |
| Additional Infomation |
Mosapride is a racemic mixture composed of equimolar amounts of (R)-mosapride and (S)-mosapride. It is a prokinetic agent that acts on 5-HT4 receptors in the gastrointestinal plexus, thereby increasing the release of acetylcholine, which in turn enhances gastrointestinal motility and gastric emptying. It is both a gastrointestinal drug and a serotonergic agonist. It contains (R)-mosapride and (S)-mosapride. Mosapride is being investigated for the treatment and prevention of postoperative intestinal obstruction and endoscopic pylorotomy (G-POEM). Mosapride has been investigated for the treatment and diagnosis of constipation, type 2 diabetes, functional dyspepsia, functional constipation and epigastric pain syndrome. Mosapride is a substituted benzamide derivative that acts primarily as a selective 5-HT4 receptor agonist and 5-HT3 receptor antagonist in the gastrointestinal tract [1].
Its main metabolite M1 has about 50% of the potency of the parent compound in stimulating gastric motility[1]. It stimulates gastrointestinal propulsion by activating 5-HT4 receptors and enhancing the release of acetylcholine from cholinergic nerve endings in the enteric nervous system[1]. In some Asian countries, it is used as a prokinetic agent to treat gastrointestinal motility disorders[1]. |
| Molecular Formula |
C21H25CLFN3O3
|
|---|---|
| Molecular Weight |
421.8929
|
| Exact Mass |
421.156
|
| CAS # |
112885-41-3
|
| Related CAS # |
Mosapride citrate;112885-42-4;Mosapride citrate dihydrate;636582-62-2;Mosapride-d5;1246820-66-5
|
| PubChem CID |
119584
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
549.2±50.0 °C at 760 mmHg
|
| Melting Point |
151-153°C
|
| Flash Point |
286.0±30.1 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.585
|
| LogP |
2.82
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
521
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1=C(C([H])=C(C(=C1[H])C(N([H])C([H])([H])C1([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])F)C([H])([H])C([H])([H])O1)=O)OC([H])([H])C([H])([H])[H])N([H])[H]
|
| InChi Key |
YPELFRMCRYSPKZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H25ClFN3O3/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/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27)
|
| Chemical Name |
4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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 | 2.3703 mL | 11.8514 mL | 23.7029 mL | |
| 5 mM | 0.4741 mL | 2.3703 mL | 4.7406 mL | |
| 10 mM | 0.2370 mL | 1.1851 mL | 2.3703 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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