Acotiamide HCl trihydrate

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Chemical Structure| 773092-05-0 同义名 : 盐酸阿考替胺 ;Acotiamide hydrochloride; YM-443 HCl; Z-338 HCl; Acotiamide monohydrochloride trihydrate
CAS号 : 773092-05-0
货号 : A254230
分子式 : C21H37ClN4O8S
纯度 : 99%
分子量 : 541.06
MDL号 : MFCD28101055
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(221.79 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 3 mg/mL(5.54 mM)，配合低频超声，并水浴加热至45℃助溶
生物活性
描述 Acotiamide hydrochloride trihydrate is a novel gastroprokinetic drug. It enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation[1]. Acotiamide inhibited AChE activity in vitro with a 50% inhibitory concentration of 1.79 μM. ACh reached the maximum concentration at 2 h after administration[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.24mL

1.85mL

0.92mL

18.48mL

3.70mL

1.85mL
参考文献

[1]Nowlan ML, Scott LJ. Acotiamide: first global approval. Drugs. 2013 Aug;73(12):1377-83. doi: 10.1007/s40265-013-0100-9. Erratum in: Drugs. 2014 Jun;74(9):1059. Nolan, Mary L [corrected to Nowlan, Mary L].

[2]Yoshii K, Iikura M, Hirayama M, Toda R, Kawabata Y. 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. Pharm Res. 2016 Feb;33(2):292-300.