Acotiamide monohydrochloride trihydrate

Name: Acotiamide monohydrochloride trihydrate
Brand: MedChemExpress
SKU: HY-B2155
Rating: 4.5 (1 reviews)

Cat. No.: HY-B2155 Purity: 99.49%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC₅₀ 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 .

For research use only. We do not sell to patients.

Acotiamide monohydrochloride trihydrate Chemical Structure

CAS No. : 773092-05-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Acotiamide monohydrochloride trihydrate:

Acotiamide-d₆ Get quote
Acotiamide Get quote
Acotiamide hydrochloride Get quote
Acotiamide monohydrochloride trihydrate (Standard) Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Cholinesterase (ChE) Isoform Specific Products:

View All Isoforms

AChE BChE

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

AChE

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^[1].

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

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 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^[2].
Acotiamide monohydrochloride trihydrate (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with IC₅₀ of 1.79 μM^[3].

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

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.

Clinical Trial

Molecular Weight

541.06

Formula

C₂₁H₃₇ClN₄O₈S

CAS No.

773092-05-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CSC(NC(C2=CC(OC)=C(OC)C=C2O)=O)=N1)NCCN(C(C)C)C(C)C.[H]Cl.O.O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (231.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 3.03 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8482 mL	9.2411 mL	18.4822 mL
5 mM	0.3696 mL	1.8482 mL	3.6964 mL
10 mM	0.1848 mL	0.9241 mL	1.8482 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.49%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (250 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[3]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.8482 mL	9.2411 mL	18.4822 mL	46.2056 mL
H₂O / DMSO	5 mM	0.3696 mL	1.8482 mL	3.6964 mL	9.2411 mL
DMSO	10 mM	0.1848 mL	0.9241 mL	1.8482 mL	4.6206 mL
	15 mM	0.1232 mL	0.6161 mL	1.2321 mL	3.0804 mL
	20 mM	0.0924 mL	0.4621 mL	0.9241 mL	2.3103 mL
	25 mM	0.0739 mL	0.3696 mL	0.7393 mL	1.8482 mL
	30 mM	0.0616 mL	0.3080 mL	0.6161 mL	1.5402 mL
	40 mM	0.0462 mL	0.2310 mL	0.4621 mL	1.1551 mL
	50 mM	0.0370 mL	0.1848 mL	0.3696 mL	0.9241 mL
	60 mM	0.0308 mL	0.1540 mL	0.3080 mL	0.7701 mL
	80 mM	0.0231 mL	0.1155 mL	0.2310 mL	0.5776 mL
	100 mM	0.0185 mL	0.0924 mL	0.1848 mL	0.4621 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.