Acotiamide
Based on 1 Customer Validation
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory.
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- Purity: 99.92%
- CAS No.: 185106-16-5
- 화학식: C21H30N4O5S
- 분자량:450.55
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
IC50: 1.79 μM (AChE)[3].
Acotiamide (10, 30, 100 μM; 1 hour) reduces expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NR8383, macrophage
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Concentration:10, 30, 100 μM
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Incubation Time:1 hour
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Result:Significantly reduced both TNF-α and IL-6 productions in LPS/MCP-1-stimulated NR8383 cells.
Acotiamide (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with an IC50 value of 1.79 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mongrel dogs (9-11 kg), Male beagle dogs (9.6-12.9 kg)[2]
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Dosage:0.3, 1, 3, 10, 30 mg/kg
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Administration:Intravenous injection; once
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Result:Increased the postprandial gastric motility.
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Animal Model:Male Sprague-Dawley rats (aged 6-7 weeks)[3]
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Dosage:0.83 mg/kg
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Administration:Intravenous injection; once.
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Result:Effectively improved functional dyspepsia by inhibiting AChE in rat stomach.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 185106-16-5
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Appearance Solid
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분자량 450.55
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화학식 C21H30N4O5S
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Color White to off-white
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SMILES
O=C(C1=CSC(NC(C2=CC(OC)=C(OC)C=C2O)=O)=N1)NCCN(C(C)C)C(C)C
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Synonyms
Z-338 free base; YM443 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 250 mg/mL (554.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Kazuyoshi Y oshii, et al. Physiologically-Based Pharmacokinetic and Pharmacodynamic Modeling for the Inhibition of Acetylcholinesterase by Acotiamide, A Novel Gastroprokinetic Agent for the Treatment of Functional Dyspepsia, in Rat Stomach. Pharmaceutical [Content Brief]
[2]. Hiroshi Yamawaki, et al. Acotiamide attenuates central urocortin 2-induced intestinal inflammatory responses, and urocortin 2 treatment reduces TNF-α productions in LPS-stimulated macrophage cell lines. Neurogastroenterol Motil. 2020 Aug;32(8):e13813. [Content Brief]
[3]. Matsunaga Y, Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride. J Pharmacol Exp Ther. 2011 Mar;336(3):791- [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2195 mL | 11.0975 mL | 22.1951 mL | 55.4877 mL |
| 5 mM | 0.4439 mL | 2.2195 mL | 4.4390 mL | 11.0975 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2195 mL | 5.5488 mL | |
| 15 mM | 0.1480 mL | 0.7398 mL | 1.4797 mL | 3.6992 mL | |
| 20 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7744 mL | |
| 25 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2195 mL | |
| 30 mM | 0.0740 mL | 0.3699 mL | 0.7398 mL | 1.8496 mL | |
| 40 mM | 0.0555 mL | 0.2774 mL | 0.5549 mL | 1.3872 mL | |
| 50 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL | |
| 60 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL | |
| 80 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6936 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5549 mL |
Acotiamide Related Classifications
HY-121467 Related Classifications
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