Nizatidine

製品コードS1890 バッチS189002

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H21N5O2S2
分子量 331.46 CAS No. 76963-41-2
Solubility (25°C)* 体外 DMSO 66 mg/mL (199.11 mM)
Water 22 mg/mL (66.37 mM)
Ethanol 5 mg/mL (15.08 mM)
* <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.

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生物活性

製品説明 Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
in vitro Nizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. [1] Nizatidine also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. [2]
in vivo Nizatidine exhibits maximal inhibition of gastric acid in rats within the first hour of drug administration, with EC50 of 1.383 μmol/kg. [1] Nizatidine (0.3-3 mg/kg, i.v.) significantly increases the motor index of gastrointestinal (GI) motility in a dose-dependent manner. Nizatidine inhibits gastric acid secretion with ED50 and ED90 of 0.18 and 3.22 mg/kg in dogs, and 2.94 and 19.6 mg/kg in rats, respectively. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Gastric acid secretion
Gastric acid secretion from the isolated bullfrog gastric mucosa is studied. The serosal buffer in this study contains 1 mM NaH2PO4. After the frog is pithed, the mucosa of the stomach is separated quickly from the muscular layers and mounted between two Lucite chambers. The serosal side of the mucosa is bathed with frog Ringer’s whereas the mucosal side with an isotonic solution containing the chlorides of Na, K and Ca ions, both of which are aerated with O2 (95%) and CO2 (5%). Acid secretion is stimulated with histamine (10 nM) in the serosal buffer which is renewed every 40 min. After a steady state is established, only one of the halves of the serosal mucosa is treated with nizatidine or the reference compound, cimetidine; the other half serves as control. The acid secretory rate is followed by maintaining the pH of the solution bathing the secretory mucosa at pH 4.5 with 0.05 N NaOH delivered from an automatic burette.
動物実験 動物モデル Rat
投薬量 0.5-10 μmol/kg
投与方法 s.c

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：

Molecular Signature Predictive of Long-Term Liver Fibrosis Progression to Inform Antifibrotic Drug Development [ Gastroenterology, 2022, 162(4):1210-1225] PubMed: 34951993
Proton Pump Inhibitors Inhibit PHOSPHO1 Activity and Matrix Mineralisation In Vitro [ Calcif Tissue Int, 2021, 109(6):696-705] PubMed: 34213594
Proton pump inhibitors inhibit PHOSPHO1 activity and matrix mineralisation in vitro [ bioRxiv, 2021, 10.1101/2021.04.29.441931] PubMed: None
Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms. [ Anticancer Res, 2019, 39(7):3767-3775] PubMed: 31262903

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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