Revaprazan Hydrochloride

For research use only.

Catalog No.S5058 Synonyms: YH1885

1 publication

Revaprazan Hydrochloride Chemical Structure

CAS No. 178307-42-1

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.

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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male Wistar rats
  • Dosages: 50 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL (40.11 mM)

* 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.

Chemical Information

Molecular Weight 398.9
Formula

C22H23FN4.HCl

CAS No. 178307-42-1
Storage powder
in solvent
Synonyms YH1885
Smiles CC1C2=CC=CC=C2CCN1C3=NC(=NC(=C3C)C)NC4=CC=C(C=C4)F.Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID