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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Acotiamide hydrochloride trihydrate (YM-443; Z-338) is a potent, orally bioactive and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. It is approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia.Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation. It acts as an acetylcholinesterase inhibitor.
| ln Vitro |
In LPS- and MCP-1-stimulated macrophage cell lines, acetamidoamide monoHClide triponder (10, 30, 100 μM; 1 hour) lowers the expression level of IκB-α phosphorylation [1].
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| ln Vivo |
In a dose-dependent manner, acocamide monohydrochloride trihydrate (0.3, 1, 3 mg/kg; iv/3, 10, 30 mg/kg; po) raises the postprandial gastric motility index [2]. With an IC50 of 1.79 μM, acotiamide monoHClide triponder (0.83 mg/kg; iv; Once) inhibits AChE in the stomach of rats [3].
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| Cell Assay |
Cell viability assay [1]
Cell Types: NR8383, macrophage Tested Concentrations: 10, 30, 100 μM Incubation Duration: 1 hour Experimental Results: The production of TNF-α and IL-6 in NR8383 cells stimulated by LPS/MCP-1 was significant reduce. |
| Animal Protocol |
Animal/Disease Models: Male mongrel dog (9-11 kg), male beagle dog (9.6-12.9 kg) [2]
Doses: 0.3, 1, 3, 10, 30 mg/kg Route of Administration: intravenous (iv) (iv)injection; once. Experimental Results: Gastric motility increased after meals. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (6-7 weeks old) [3] Doses: 0.83 mg/kg Route of Administration: intravenous (iv) (iv)injection; once. Experimental Results: Functional dyspepsia was effectively improved by inhibiting AChE in the stomach of rats. |
| References |
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| Additional Infomation |
Acotiamide Hydrochloride is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms.
See also: Acotiamide (annotation moved to). |
| Molecular Formula |
C21H37CLN4O8S
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|---|---|
| Molecular Weight |
541.0585
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| Exact Mass |
540.202
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| CAS # |
773092-05-0
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| Related CAS # |
Acotiamide;185106-16-5;Acotiamide hydrochloride;185104-11-4;Acotiamide-d6
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| PubChem CID |
6918406
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.534
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
586
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NPTDXIXCQCFGKC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H30N4O5S.ClH.3H2O/c1-12(2)25(13(3)4)8-7-22-20(28)15-11-31-21(23-15)24-19(27)14-9-17(29-5)18(30-6)10-16(14)26/h9-13,26H,7-8H2,1-6H3,(H,22,28)(H,23,24,27)1H3*1H2
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| Chemical Name |
N-(2-(diisopropylamino)ethyl)-2-(2-hydroxy-4,5-dimethoxybenzamido)thiazole-4-carboxamide hydrochloride trihydrate.
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| Synonyms |
Z338 Z-338 Z 338YM443 YM-443 YM 443 Acotiamide Acotiamide hydrochloride trihydrate Acofide.
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~231.03 mM)
H2O : ~3.03 mg/mL (~5.60 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.84 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 20.8 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: ≥ 2.08 mg/mL (3.84 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 20.8 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: ≥ 2.08 mg/mL (3.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8482 mL | 9.2411 mL | 18.4822 mL | |
| 5 mM | 0.3696 mL | 1.8482 mL | 3.6964 mL | |
| 10 mM | 0.1848 mL | 0.9241 mL | 1.8482 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 |
| NCT00764374 | Completed | Drug: YM443 | Dyspepsia Functional Dyspepsia |
Astellas Pharma Inc | August 2008 | Phase 3 |
| NCT00850746 | Completed | Drug: YM443 Drug: Placebo |
Functional Dyspepsia | Astellas Pharma Inc | February 2009 | Phase 1 |
| NCT00920998 | Completed | Drug: Z-338 | Healthy | Astellas Pharma Inc | March 2009 | Phase 1 |
| NCT01973790 | Completed | Drug: Z-338 | Dyspepsia | Zeria Pharmaceutical | March 2014 | Phase 3 |
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