Acotiamide monohydrochloride trihydrate|773092-05-0|(盐酸阿考替胺三水合物)-陌孚医药/Medlife

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Acotiamide monohydrochloride trihydrate (Synonyms: 盐酸阿考替胺三水合物)

目录号: PL05579 纯度: ≥99%

CAS No. :773092-05-0

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中文名称	Acotiamide monohydrochloride trihydrate
中文别名	盐酸阿考替胺三水合物;盐酸阿考替胺;三水合盐酸阿卡替胺;三水合阿替考胺盐酸盐;N-{2 - [双(1-甲基乙基)氨基]乙基} -2 -[(2-羟基-4,5 - 二甲氧基苯甲酰基)氨基]-噻唑-4-甲酰胺单盐酸盐三水合物;盐酸阿考替胺三水合物ACOTIAMIDE HCL;盐酸阿考替胺三水化合物;2-[N-(4,5-二甲氧基-2-羟基苯甲酰基)氨基]-4-（乙氧基羰基）-1,3-噻唑乙酸盐;盐酸阿考替胺三水物;盐酸阿考替胺杂质
英文名称	Acotiamide monohydrochloride trihydrate
英文别名	Acotiamide hydrochloride trihydrate;Acotiamide HCl;Acotiamide hydrochloride hydrate;N-(2-(Diisopropylamino)ethyl)-2-((2-hydroxy-4,5-dimethoxybenzoyl)amino)-1,3-thiazole-4-carboxyamide monohydrochloride trihydrate;Unii-nmw7447A9a;Ym-443;Acotiae;4-Thiazolecarboxamide, N-[2-[bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-,hydrochloride,hydrate(1:1:3);Acotiamidehydrochloride;N-[2-[di(propan-2-yl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide,trihydrate,hydrochloride;Acofide;Z-338;Acofide trihydrate;NMW7447A9A;Acotiamide hydrochloride [USAN];YM443;Acotiamide hydrochloride (USAN);N-(2-(diisopropylamino)ethyl)-2-(2-hydroxy-4,5-dimethoxybenzamido)thiazole-4-carboxamide hydrochloride trihydrate;N-[2-(Diisopropylamino)ethyl]-2-(2-hydroxy-4,5-dimethoxybenzamido)thiazole-4-carboxamide Hydrochloride Trihydrate;acotiamide-hydrochloride;Acotiamide monohydrochloride trihydrate
Cas No.	773092-05-0
分子式	C₂₁H₃₇ClN₄O₈S
分子量	541.06
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

Acotiamide monohydrochloride trihydrate 是一种口服有效的、具有选择性和可逆性的乙酰胆酶碱酯 (AChE) 抑制剂,其 IC₅₀ 值为1.79 μM。Acotiamide monohydrochloride trihydrate 可增强胃收缩性并加速胃排空延迟。Acotiamide monohydrochloride trihydrate 可用于胃动力障碍的功能性消化不良及肠道炎症的研究。

生物活性

Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC 50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .

性状

Solid

IC50 & Target[1][2]

AChE

体外研究(In Vitro)

Acotiamide monohydrochloride trihydrate (10, 30, 100 μM; 1 hour) reduces expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

体内研究(In Vivo)

Acotiamide monohydrochloride trihydrate (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.
Acotiamide monohydrochloride trihydrate (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with IC 50 of 1.79 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. 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.
[2]. Matsunaga Y, et al. 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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (231.03 mM; Need ultrasonic)H₂O : 3.03 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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