Acotiamide-monohydrochloride-trihydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAcotiamide monohydrochloride trihydrateCat. No.: HY-B2155CAS No.: 773092-05-0分式: CHClNOS分量: 541.06作靶點(diǎn): AChE作通路: Neuronal Signaling儲存式: 4C, sealed storage, away from moisture and light* In solvent : -80C, 6 months; -20C, 1 month

2、(sealedstorage, away from moisture and light)溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (231.03 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.8482 mL 9.2411 mL 18.4822 mL5 mM 0.3696 mL 1.8482 mL 3.6964 mL10 mM 0.1848 mL 0.9241 mL 1.8482 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請

3、根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.84 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.84

4、 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.84 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Acotiamide monohydrochloride trihydrate種服活性和流的于治療功能性消化不良的胃腸動藥。Acotiamide monohydrochloride trihydrate 通過促毒蕈堿受體拮抗作和酰膽堿酯酶 (AChE

5、) 抑制作增強(qiáng)腸神經(jīng)元釋放的酰膽堿，從增強(qiáng)胃排空和胃部適應(yīng)性。體外研究 In in vitro studies, Acotiamide inhibits acetylcholine-induced activation of muscarinic M1 and M2 receptors intransformed Xenopus oocytes, with IC50 values of 1.8 and 10.1 M, respectively. Acotiamide showsno/limited affinity for serotonin 5HT2, 5HT3 or 5HT4 recept

6、ors and dopamine D2 receptors 1.Acotiamide inhibits AChE activity, inhibits both the slow (competitively) and fast (noncompetitively) inwardcurrents induced by acetylcholine, enhances electrically stimulated contraction of gastric fundus and gastricbody, facilitates acetylcholine release from enteri

7、c neurons and, using patch-clamp techniques, potentiates L-type voltagedependent Ca2+ current and inhibits GABA-induced current in area postrema neurons 1.體內(nèi)研究 In in vivo animal models, Acotiamide stimulates postprandial gastroduodenal and/or colonic motor activity,and improves delayed but not norma

8、l gastric emptying. For example, Acotiamide significantly improvesdelayed gastric emptying and feeding inhibition in a restraintstress-induced rat model, but does not affectnormal gastric emptying or feeding in intact rats 1.REFERENCES1. Nowlan ML, et al. Acotiamide: first global approval. Drugs. 2013 Aug;73(12):1377-83.2. Attia KAM, et al. Spectrofluorimetric determination of acotiamide hydrochloride trihydrate in the presence of its oxidative degradationproduct. Luminescence. 2018 Jun;33(4):806-811.McePdfHeightCaution: Product has not been fully validated for medical ap