DC Chemicals Limited
China
Product Name: Acotiamide
Price: $200.0/100mg $400.0/250mg $800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

185106-16-5

185106-16-5 structure

Name: Acotiamide
Chemical Name: N-[2-[di(propan-2-yl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide
CAS Number: 185106-16-5
Molecular Formula: C₂₁H₃₀N₄O₅S
Molecular Weight: 450.552
Catalog: Signaling Pathways Neuronal Signaling AChE
Create Date: 2018-05-23 08:00:00
Modify Date: 2024-01-02 17:47:46
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with 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].

Name	N-[2-[di(propan-2-yl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide
Synonyms	Acotiamide MZ-338 N-[2-(Diisopropylamino)ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide UNII-D42OWK5383 4-Thiazolecarboxamide, N-[2-[bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-

Description	Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with 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].
Related Catalog	Research Areas >> Inflammation/Immunology Research Areas >> Metabolic Disease Signaling Pathways >> Neuronal Signaling >> AChE
Target	IC50: 1.79 μM (AChE)
In Vitro	Acotiamide (10, 30, 100 μM; 1 hour) reduces expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines[1]. Cell Viability Assay[1] Cell Line: NR8383, macrophage Concentration: 10, 30, 100 μM Incubation Time: 1 hour Result: Significantly reduced both TNF-α and IL-6 productions in LPS/MCP-1-stimulated NR8383 cells.
In Vivo	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 IC50 of 1.79 μM[3]. Animal Model: Male mongrel dogs (9-11 kg), Male beagle dogs (9.6-12.9 kg)[2] Dosage: 0.3, 1, 3, 10, 30 mg/kg Administration: Intravenous injection; once Result: Increased the postprandial gastric motility. Animal Model: Male Sprague-Dawley rats (aged 6-7 weeks)[3] Dosage: 0.83 mg/kg Administration: Intravenous injection; once. Result: Effectively improved functional dyspepsia by inhibiting AChE in rat stomach.
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 Research, 33(2), 292–300. [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. [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):791-800.

Density	1.2±0.1 g/cm3
Molecular Formula	C₂₁H₃₀N₄O₅S
Molecular Weight	450.552
Exact Mass	450.193695
PSA	148.24000
LogP	3.56
Index of Refraction	1.592
Storage condition	-20℃

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