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Details

Stereochemistry ACHIRAL
Molecular Formula C21H26N4O2
Molecular Weight 366.4567
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LINAPRAZAN

SMILES

CC1=C(C)N2C=C(C=C(NCC3=C(C)C=CC=C3C)C2=N1)C(=O)NCCO

InChI

InChIKey=GHVIMBCFLRTFHI-UHFFFAOYSA-N
InChI=1S/C21H26N4O2/c1-13-6-5-7-14(2)18(13)11-23-19-10-17(21(27)22-8-9-26)12-25-16(4)15(3)24-20(19)25/h5-7,10,12,23,26H,8-9,11H2,1-4H3,(H,22,27)

HIDE SMILES / InChI

Description

Linaprazan is a member of a new group of acid-suppressing agents, which unlike proton pump inhibitors, act through potassium-competitive inhibition of the H+,K+-ATPase located in the apical membrane of parietal cells. It displayed rapid inhibition of acid production and had a prolonged, dose-dependent duration of effect. Linaprazan reduced porcine renal Na(+),K(+)-ATPase activity by 9+/-2%, demonstrating a high selectivity for H(+),K(+)-ATPase. It provided similar efficacy to esomeprazole in terms of esophagitis healing and heartburn control.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.13 µM [IC50]

PubMed

Sample Use Guides

In Vivo Use Guide
25, 50, 75 mg given once daily for 4 weeks
Route of Administration: Oral