Home Neuronal Signaling AChR inhibitor Acotiamide For research use only.

Acotiamide

Synonyms: Acofide, Z388

Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.

Acotiamide Chemical Structure

Acotiamide Chemical Structure

CAS: 185106-16-5

Purity & Quality Control

Batch: S507501 DMSO] 90 mg/mL] false] Ethanol] 38 mg/mL] false] Water] Insoluble] false Purity: 99.01%
99.01

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Biological Activity

Description Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
Targets
AChE [2]
3 μM
In vitro
In vitro Acotiamide inhibited recombinant human and canine stomach-derived acetylcholinesterase (AChE) activity in vitro. The mode of the AChE inhibitory action of acotiamide was selective and reversible. It shows a mixed-type inhibition toward recombinant human AChE activity. Ki1 (competitive inhibition) and Ki2 values (noncompetitive inhibition) of acotiamide were 610 nM and 2.7 μM, respectively. IC50 values for AChE of acotiamide is 3 μM. IC50 value for BuChE of acotiamide is >1.0 × 10−3 M. Acotiamide inhibited AChE selectively, and the ratio of the IC50 value for BuChE to AChE was more than 330. Acotiamide has no affinity for α2-adrenoceptor, dopamine D2S receptor, or serotonin 5-HT4 receptors, including 5-HT4c, 5-HT4d, or 5-HT4e receptors. In in vitro studies, acotiamide enhanced acetylcholine- but not carbachol-induced contractile responses of guinea pig gastric antrum strips[2].
In Vivo
In vivo Acotiamide stimulates gastric motility and improves gastric motility dysfunction in rats by inhibiting AChE activity. It improves stress-induced delayed gastric emptying in rats. Acotiamide also enhances gastric motility by inhibiting AChE activity without affecting QT interval in dogs[1].
Animal Research Animal Models Male Sprague-Dawley rats aged 7 to 9 weeks
Dosages 10, 30, and 100 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 450.55 Formula

C21H30N4O5S
CAS No. 185106-16-5 SDF --
Smiles CC(C)N(CCNC(=O)C1=CSC(=N1)NC(=O)C2=CC(=C(C=C2O)OC)OC)C(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (199.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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