Cisapride hydrate

製品コードS4751 バッチS475102

印刷

化学情報

Chemical Structure Synonyms Propulsid, Alimix, Propulsin, Enteropride, Kinestase Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H29ClFN3O4.H2O
分子量 483.96 CAS No. 260779-88-2
Solubility (25°C)* 体外 DMSO 97 mg/mL (200.42 mM)
Water Insoluble
Ethanol 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 Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
in vitro Cisapride inhibits vascular Kv current independently of serotonin 5-HT4-receptor activation[2]. As HERG channel blocker, cisapride, can inhibit the growth of gastric cancer cells by altering distribution of cell cycle and inducing apoptosis so as to be of potential value in the treatment of gastric cancer. Cisapride could inhibit the growth and clonogenicity of human gastric cancer lines by specific blockage of HERG channel in a time- and dose-dependent manner while has little effects on GES cells[3].
in vivo Cisapride is widely prescribed for the treatment of gastrointestinal motility dysfunctions, such as gastroesophageal reflux disorder (GERD), chronic intestinal pseudo-obstruction, and slow-transit constipation gastroparesis. Although cisapride is a beneficial prokinetic agent, several common side effects, such as abdominal pain, nausea, diarrhea, and increased frequency of urination, have been reported[2]. In rat, the PK profile indicate the T1/2 for cisapride is 1.48 h[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The human gastric cancer SGC7901, AGS, MGC803 and MKN45 cell lines and human immortalized gastric epithelial GES cell line
濃度 0, 12.5, 25, 50, 100 or 200 nM
反応時間 1, 3, 5 and 7 day
実験の流れ Cells in the logarithmic growth phase are harvested and seeded in 96-well plates. The cell number is diluted to 5000/well in 200 microliters of RPMI1640 medium. In vitro experiments are carried out on the gastric cancer cell lines and GES cell line, using an MTT proliferation assay. MTT stains live cells, and the optical density absorbance at 490nm wavelength correlates with the cell number. Cisapride is added to the cells at concentrations of 0, 12.5, 25, 50, 100 or 200 nM and equivalent volume of ethanol is added as control in order to eliminate the effects of solvent. Twenty microliters of MTT is added to each well of the cell culture 4 h before termination of the culture at 37˚C. One hundred and fifty microliters of dimethyl sulfoxide is added to each well at the end of the culture and the plate is agitated for 10 minutes. The absorbency at 490 nm is read by a BIOHIT BP800 plate reader. Growth curve is drawn according to MTT colorimetry. The inhibition rate is calculated.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 5 mg/kg
投与方法 i.v.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Deep learning detects cardiotoxicity in a high-content screen with induced pluripotent stem cell-derived cardiomyocytes [ Elife, 2021, 10e68714] PubMed: 34338636

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。

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