Home Transmembrane Transporters Proton Pump inhibitor - ATPase inhibitor Dexlansoprazole

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Dexlansoprazole Proton Pump inhibitor

Cat.No.S4099

Dexlansoprazole (T 168390, TAK 390,(R)-Lansoprazole), the dextrorotatory enantiomer of lansoprazole, is a proton pump inhibitor (PPI) formulated to have dual delayed-release properties. This compound selectively suppresses gastric acid secretion by direct inhibition of the H(+),K(+)-ATPase proton pump in the gastric parietal cell.
Dexlansoprazole Proton Pump inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 369.36

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

Quality Control

Batch: S409901 DMSO]74 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.92%
99.92

Chemical Information, Storage & Stability

Molecular Weight 369.36 Formula

C16H14F3N3O2S

 Storage (From the date of receipt)
CAS No. 138530-94-6 Download SDF Storage of Stock Solutions

Synonyms T 168390, TAK 390,(R)-Lansoprazole Smiles CC1=C(C=CN=C1CS(=O)C2=NC3=CC=CC=C3N2)OCC(F)(F)F

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (200.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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.

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Mechanism of Action

Features
A modified release formulation of an enantiomer of lansoprazole.
Targets/IC50/Ki
Proton pump [1]
H(+),K(+)-ATPase [1]
In vitro

Dexlansoprazole, constitutes >80% of circulating drug after oral administration of lansoprazole, provides lower clearance and 5-fold greater systemic exposure than the S-enantiomer following oral administration of lansoprazole. This compound MR is a modified release formulation of dexlansoprazole, which employs a novel Dual Delayed Release (DDR) technology that delivers the drug in two discrete phases of release, thereby inhibiting newly activated proton pumps that turn over following initial PPI inactivation of H+,K+-ATPase. This formulation maintains plasma drug concentrations above the threshold level longer than lansoprazole at all doses, resulting in an optimized drug exposure-intragastric pH relationship. [1] It selectively suppresses gastric acid secretion by direct inhibition of the H+K+-ATPase proton pump in the gastric parietal cell, inhibition of this cell membrane enzyme ultimately blocks the final step in acid production. [2]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02442752 Withdrawn
Pediatric Gastroesophageal Reflux Disease
Takeda
 June 15 2025 Phase 1
NCT03316976 Completed
Healthy Volunteers
Takeda
 November 22 2017 Phase 1
NCT03079050 Completed
GERD|Proton Pump Inhibitor
American University of Beirut Medical Center|Takeda
 February 27 2017 Phase 4

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