Itopride hydrochloride
Based on 1 Customer Validation
Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 122892-31-3
- Formula: C20H27ClN2O4
- Molecular Weight:394.89
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Dopamine Receptor Isoforms
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Biological Activity
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D2 Receptor |
AChE |
Itopride hydrochloride has prokinetic effects on both the ileum and colon, which are regulated through inhibitory effects on AChE and antagonistic effects on dopamine D2 receptor[3].
Itopride hydrochloride (0.1 nM-1 μM) significantly accelerats the propagation velocity of the peristalsis in ex guinea pig ileum[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Itopride hydrochloride (30 mg/kg; p.o.) displays Cmax of 358 ‰, T1/2 of 24.9 min[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ddY-strain mice (23.7-28.5 g)[2]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration
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Result:Accelerated gastric emptying at 30 mg/kg dose.
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Animal Model:Male ddY-strain mice (23.7-28.5 g)[2]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral administration
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Result:Cmax (358 ‰), T1/2 (24.9 min) at 30 mg/kg dose.
Chemical Information
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CAS No. 122892-31-3
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Appearance Solid
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Molecular Weight 394.89
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Formula C20H27ClN2O4
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Color White to off-white
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SMILES
O=C(NCC1=CC=C(OCCN(C)C)C=C1)C2=CC=C(OC)C(OC)=C2.Cl
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Synonyms
HSR803
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (253.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (126.62 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.33 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 (6.33 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (253.24 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 KB)
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Handling Instructions (2659 KB)
References
[1]. Iwanaga Y, et al. A novel water-soluble dopamine-2 antagonist with anticholinesterase activity in gastrointestinal motor activity. Comparison with domperidone and neostigmine. Gastroenterology. 1990 Aug;99(2):401-8. [Content Brief]
[2]. Kim YS, et al. Effect of itopride, a new prokinetic, in patients with mild GERD: a pilot study. World J Gastroenterol. 2005 Jul 21;11(27):4210-4. [Content Brief]
[3]. Hyun Chul Lim, et al. Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro. Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro. Yonsei Med J. 2008 Jun 30;49(3):472-8. [Content Brief]
[4]. Kenjiro Matsumoto, et al. Validation of 13 C-Acetic Acid Breath Test by Measuring Effects of Loperamide, Morphine, Mosapride, and Itopride on Gastric Emptying in Mice. Biol Pharm Bull. 2008 Oct;31(10):1917-22. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.5324 mL | 12.6618 mL | 25.3235 mL | 63.3088 mL |
| 5 mM | 0.5065 mL | 2.5324 mL | 5.0647 mL | 12.6618 mL | |
| 10 mM | 0.2532 mL | 1.2662 mL | 2.5324 mL | 6.3309 mL | |
| 15 mM | 0.1688 mL | 0.8441 mL | 1.6882 mL | 4.2206 mL | |
| 20 mM | 0.1266 mL | 0.6331 mL | 1.2662 mL | 3.1654 mL | |
| 25 mM | 0.1013 mL | 0.5065 mL | 1.0129 mL | 2.5324 mL | |
| 30 mM | 0.0844 mL | 0.4221 mL | 0.8441 mL | 2.1103 mL | |
| 40 mM | 0.0633 mL | 0.3165 mL | 0.6331 mL | 1.5827 mL | |
| 50 mM | 0.0506 mL | 0.2532 mL | 0.5065 mL | 1.2662 mL | |
| 60 mM | 0.0422 mL | 0.2110 mL | 0.4221 mL | 1.0551 mL | |
| 80 mM | 0.0317 mL | 0.1583 mL | 0.3165 mL | 0.7914 mL | |
| 100 mM | 0.0253 mL | 0.1266 mL | 0.2532 mL | 0.6331 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Itopride hydrochloride Related Classifications
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