| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
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| ln Vitro |
The prokinetic action of icopride hydrochloride is regulated by the antagonistic effect on dopamine D2 receptors and the inhibitory effect on AChE in both the colon and the ileum [3]. In the ileum of guinea pigs, itopride hydrochloride (0.1 nM-1 μM) dramatically increases the rate of peristalsis propagation [3].
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| ln Vivo |
In comparison to the vehicle group, itopride hydrochloride (30 mg/kg; oral) dramatically accelerated stomach emptying [4]. Oral ilopride hydrochloride (30 mg/kg) exhibits a T1/2 of 24.9 min and a Cmax of 358 ‰ [4].
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| Animal Protocol |
Animal/Disease Models: Male ddY strain mouse (23.7-28.5 g) [2]
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: Oral Experimental Results:Accelerated gastric emptying at 30 mg/kg dose . Animal/Disease Models: Male ddY strain mouse (23.7-28.5 g) [2] Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Oral Experimental Results:Cmax (358 ‰), T1 /2 (24.9 minutes), dose 30 mg/kg. |
| References |
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| Molecular Formula |
C20H27CLN2O4
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|---|---|
| Molecular Weight |
394.89
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| Exact Mass |
394.165
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| CAS # |
122892-31-3
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| Related CAS # |
Itopride;122898-67-3;Itopride-d6 hydrochloride;1346601-02-2
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| PubChem CID |
129791
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| Appearance |
White to off-white solid powder
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| Boiling Point |
510.1ºC at 760 mmHg
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| Melting Point |
194-1950ºC
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| Flash Point |
262.3ºC
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| Vapour Pressure |
1.6E-10mmHg at 25°C
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| LogP |
3.767
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
27
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| Complexity |
411
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZTOUXLLIPWWHSR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H26N2O4.ClH/c1-22(2)11-12-26-17-8-5-15(6-9-17)14-21-20(23)16-7-10-18(24-3)19(13-16)25-4;/h5-10,13H,11-12,14H2,1-4H3,(H,21,23);1H
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| Chemical Name |
N-[[4-[2-(dimethylamino)ethoxy]phenyl]methyl]-3,4-dimethoxybenzamide;hydrochloride
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| Synonyms |
N-((4-(2-(Dimethylamino)ethoxy)phenyl)methyl)-3,4-dimethoxybenzamide monohydrochlorideItopride hydrochlorideHSR803 HSR-803HSR 803
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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) |
DMSO : ~100 mg/mL (~253.24 mM)
H2O : ~50 mg/mL (~126.62 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (253.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5324 mL | 12.6618 mL | 25.3235 mL | |
| 5 mM | 0.5065 mL | 2.5324 mL | 5.0647 mL | |
| 10 mM | 0.2532 mL | 1.2662 mL | 2.5324 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00112203 | COMPLETED | Drug: Itopride | Dyspepsia | Forest Laboratories | 2004-11 | Phase 3 |
| NCT00110968 | COMPLETED | Drug: Itopride hydrochloride | Dyspepsia | Forest Laboratories | 2004-09 | Phase 3 |
| NCT01332890 | COMPLETED | Other: Sequence 1 Other: Sequence 2 Other: Sequence 3 |
Healthy | Yuhan Corporation | 2011-04 | Phase 1 |
| NCT00112190 | COMPLETED | Drug: Itopride Hydrochloride Drug: itopride |
Dyspepsia | Forest Laboratories | 2004-07 | Phase 3 |
| NCT00112177 | COMPLETED | Drug: Itopride Hydrochloride | Dyspepsia | Forest Laboratories | 2004-07 | Phase 3 |
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