Revaprazan Hydrochloride

製品コードS5058 バッチS505801

化学情報

	Synonyms	YH1885	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₂₃FN₄.HCl
	分子量	398.9	CAS No.	178307-42-1
Solubility (25°C)*	体外	DMSO	16 mg/mL (40.11 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	Revaprazan Hydrochloride (YH1885) is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. Revaprazan Hydrochloride reversibly inhibits H(+)/K(+)-ATPase via binding to the K+-binding site of the pump.
in vitro	Revaprazan Hydrochloride reversibly inhibits H+/K+-ATPase via binding to the K+-binding site of the pump. This reversibility leads to fewer adverse events^[1]. 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^[2].
in vivo	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^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	AGS cells, human gastric adenocarcinoma epithelial cell
	濃度	5, 20, 50 μM
	反応時間	2 h
	実験の流れ	AGS cells pretreated for 2 h with vehicle or revaprazan (5, 20, 50 μM, respectively) were incubated in the presence of H. pylori for 24 h for determination of protein levels of COX-2 and Akt. To check the LPS-stimulated expression of COX2 and IκBα, AGS cells were treated H.pylori after 2 h revaprazan pretreatment. Medium was washed out twice with ice-cold PBS before harvesting the cell lysates. The nuclei and cytosolic proteins were separated from the pellets. AGS cells were lysed in RIPA lysis buffer for 15 min at 0℃ followed by centrifugation at 13,000×g for 15 min. The protein concentration of the supernatant was measured by using the BCA reagents.
動物実験	動物モデル	Male Wistar rats
	投薬量	50 mg/kg
	投与方法	oral

参考

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：

A Machine Learning Strategy for Drug Discovery Identifies Anti-Schistosomal Small Molecules [ ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754]	PubMed: 33434015

A Machine Learning Strategy for Drug Discovery Identifies Anti-Schistosomal Small Molecules [ ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754]

PubMed: 33434015

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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