1. Neuronal Signaling
  2. AChE
  3. Acotiamide monohydrochloride trihydrate

Acotiamide monohydrochloride trihydrate 

Cat. No.: HY-B2155 Purity: 99.28%
Handling Instructions

Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation.

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

Acotiamide monohydrochloride trihydrate Chemical Structure

Acotiamide monohydrochloride trihydrate Chemical Structure

CAS No. : 773092-05-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation[1][2].

In Vitro

In in vitro studies, Acotiamide inhibits acetylcholine-induced activation of muscarinic M1 and M2 receptors in transformed Xenopus oocytes, with IC50 values of 1.8 and 10.1 μM, respectively. Acotiamide shows no/limited affinity for serotonin 5HT2, 5HT3 or 5HT4 receptors and dopamine D2 receptors[1].
Acotiamide inhibits AChE activity, inhibits both the slow (competitively) and fast (noncompetitively) inward currents induced by acetylcholine, enhances electrically stimulated contraction of gastric fundus and gastric body, facilitates acetylcholine release from enteric neurons and, using patch-clamp techniques, potentiates L-type voltagedependent Ca2+ current and inhibits GABA-induced current in area postrema neurons[1].

In Vivo

In in vivo animal models, Acotiamide stimulates postprandial gastroduodenal and/or colonic motor activity, and improves delayed but not normal gastric emptying. For example, Acotiamide significantly improves delayed gastric emptying and feeding inhibition in a restraintstress-induced rat model, but does not affect normal gastric emptying or feeding in intact rats[1].

Clinical Trial
Molecular Weight

541.06

Formula

C₂₁H₃₇ClN₄O₈S

CAS No.

773092-05-0

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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Acotiamide monohydrochlorideAChEAcetylcholinesteraseInhibitorinhibitorinhibit

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Product name:
Acotiamide monohydrochloride trihydrate
Cat. No.:
HY-B2155
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