Acotiamide

Catalog No.S5075 Batch:S507501

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Technical Data

Formula

C21H30N4O5S

Molecular Weight 450.55 CAS No. 185106-16-5
Solubility (25°C)* In vitro DMSO 90 mg/mL (199.75 mM)
Ethanol 38 mg/mL (84.34 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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 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].

Protocol (from reference)

Animal Study:

[1]

  • Animal Models

    Male Sprague-Dawley rats aged 7 to 9 weeks

  • Dosages

    10, 30, and 100 mg/kg

  • Administration

    s.c.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.