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- Revaprazan HCl 178307-42-1
- Revaprazan HCl 178307-42-1
Revaprazan HCl 178307-42-1
产品描述 描述 Revaprazan Hydrochloride is the hydrochloride salt form of a lipophilic, weak base with potassium-competitive acid blocking (P-CAB) activity. Revaprazan concentrates highly in the gastric parietal cell canaliculus and on entering this acidic environment is instantly protonated and binds competitively and reversibly to the potassium binding site of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.
纯度 99%储存/保存方法 Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.基本信息 可溶性/溶解性 10 mM in DMSO生物活性 靶点 Proton pumpIn vitro(体外研究) Revaprazan Hydrochloride reversibly inhibits H+/K+-ATPase via binding to the K+-binding site of the pump. This reversibility leads to fewer adverse events. Revaprazan could inhibit H.pylori-induced COX-2 expression by blocking phosphorylation of IκB-α and Akt signaling in AGS cells. It could impose significant anti-inflammatory actions on H.pylori infection beyond acid suppression.In vivo(体内研究) Pharmacokinetic studies of revaprazan hydrochloride in rats and dogs showed the drug had a low oral bioavailability, which was speculated to be due to first pass effect and poor water solubility of drug.参考文献 参考文献 1. Lee JS, et al.J Clin Biochem Nutr. 2012 Sep;51(2):77-83.
2. Jung JW, et al. Tohoku J Exp Med. 2011;224(4):293-300.
研究领域 研究领域 MetabolismTypes of diseaseDrug DiscoverySmall Molecule DrugLead Compound DiscoveryRevaprazan HCl 178307-42-1温馨提示：本产品仅作科研实验使用，不支持临床等研究