Acotiamide  (Synonyms: Z-338 free base; YM443 free base)

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^[1][2][3].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Acotiamide (0.3, 1, 3 mg/kg; i.v./3, 10, 30 mg/kg; p.o.) increases the postprandial gastric motility index in a dose-dependent manner^[2].
Acotiamide (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with an IC₅₀ value of 1.79 μM^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

450.55

C₂₁H₃₀N₄O₅S

185106-16-5

阿考替胺杂质27

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]