Revaprazan Hydrochloride

Catalog No.S5058 Synonyms: YH1885

For research use only.

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.

Revaprazan Hydrochloride Chemical Structure

CAS No. 178307-42-1

Selleck's Revaprazan Hydrochloride has been cited by 1 Publication

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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 Research:

[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 Research:

[1]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 398.9
Formula

C22H23FN4.HCl

CAS No. 178307-42-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C2=CC=CC=C2CCN1C3=NC(=NC(=C3C)C)NC4=CC=C(C=C4)F.Cl

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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