Acotiamide

製品コードS5075 バッチS507501

化学情報

	Synonyms	Acofide, Z388	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₃₀N₄O₅S
	分子量	450.55	CAS No.	185106-16-5
Solubility (25°C)*	体外	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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

動物実験	動物モデル	Male Sprague-Dawley rats aged 7 to 9 weeks
	投薬量	10, 30, and 100 mg/kg
	投与方法	s.c.

参考

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。