Revaprazan Hydrochloride

Catalog No.S5058 Batch:S505801

Technical Data

Formula	C₂₂H₂₃FN₄.HCl
Molecular Weight	398.9	CAS No.	178307-42-1
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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.

Targets

Proton pump ^[1]

H(+)/K(+)-ATPase ^[1]

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].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines AGS cells, human gastric adenocarcinoma epithelial cell Concentrations 5, 20, 50 μM Incubation Time 2 h Method 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.
Animal Study:^{^[1]}	Animal Models Male Wistar rats Dosages 50 mg/kg Administration oral

Cell Assay:^{^[2]}

Cell lines
AGS cells, human gastric adenocarcinoma epithelial cell
Concentrations
5, 20, 50 μM
Incubation Time
2 h
Method
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.

Animal Study:^{^[1]}

Animal Models
Male Wistar rats
Dosages
50 mg/kg
Administration
oral

References

Selleck's Revaprazan Hydrochloride has been cited by 1 publication

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

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SHIPPING AND STORAGE
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