Home Transmembrane Transporters Proton Pump inhibitor - ATPase inhibitor Revaprazan Hydrochloride

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Revaprazan Hydrochloride Proton Pump inhibitor

Cat.No.S5058

Revaprazan Hydrochloride (YH1885) is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. This compound reversibly inhibits H(+)/K(+)-ATPase via binding to the K+-binding site of the pump.
Revaprazan Hydrochloride Proton Pump inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 398.9

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S505801 DMSO]16 mg/mL]false]Water]Insoluble]false]]]false Purity: 99.99%
99.99

Chemical Information, Storage & Stability

Molecular Weight 398.9 Formula

C22H23FN4.HCl

 Storage (From the date of receipt)
CAS No. 178307-42-1 -- Storage of Stock Solutions

Synonyms YH1885 Smiles CC1C2=CC=CC=C2CCN1C3=NC(=NC(=C3C)C)NC4=CC=C(C=C4)F.Cl

Solubility

In vitro
Batch:

DMSO : 16 mg/mL (40.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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]. This compound 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 this compound[1].
References

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