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Linaprazan

CAT: 0804-HY-100412-06Size: 100 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-100412-06Size:100 mg
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Description
Linaprazan (AZD0865) can inhibit H+, K+ -ATPase in the stomach through K+ competitive binding, (IC50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid. Linaprazan (AZD0865) can be used for research on reflux esophagitis with oral activity[1][2][3].
CAS Number
248919-64-4
Product Name Alternative
AZD0865
UNSPSC
12352005
Hazard Statement
H302-H315-H319
Target
Proton Pump
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/AZD0865.html
Concentration
10mM
Purity
98.80
Solubility
DMSO : ≥ 35 mg/mL
Smiles
O=C(C1=CN2C(C(NCC3=C(C)C=CC=C3C)=C1)=NC(C)=C2C)NCCO
Molecular Formula
C21H26N4O2
Molecular Weight
366.46
Precautions
P264-P270-P280-P302+P352-P305+P351+P338-P330-P362+P364-P501
References & Citations
[1]Gedda K et al. Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+, K+-ATPase. Biochem Pharmacol. 2007 Jan 15;73 (2) :198-205.|[2]Kahrilas PJ et al. A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis. Clin Gastroenterol Hepatol. 2007 Dec;5 (12) :1385-91.|[3]Xinyue Zhang, et al. Absorption, distribution, metabolism and excretion of linaprazan glurate in rats. J Pharm Biomed Anal. 2024 May 15:242:116012.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2

Chemical Information

Linaprazan

Linaprazan is a small molecule drug. The usage of the INN stem '-prazan' in the name indicates that Linaprazan is a proton pump inhibitor, not dependent on acid activation. Linaprazan is under investigation in clinical trial NCT00206284 (A Dose-finding Phase IIb Study With AZD0865 and Esomeprazole in GERD Patients Without Erosive Esophagitis.). Linaprazan has a monoisotopic molecular weight of 366.21 Da.

CAS Number248919-64-4
PubChem CID9951066
IUPAC Name8-[(2,6-dimethylphenyl)methylamino]-N-(2-hydroxyethyl)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
Molecular FormulaC21H26N4O2
Molecular Weight366.5
XLogP3.4
Topological Polar Surface Area78.7
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count4
Rotatable Bond Count6
Heavy Atom Count27
Formal Charge0
Complexity493
SMILES
CC1=C(C(=CC=C1)C)CNC2=CC(=CN3C2=NC(=C3C)C)C(=O)NCCO
InChI
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)
InChIKey
GHVIMBCFLRTFHI-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Linaprazan
CAS: 248919-64-4
CID: 9951066
Formula: C21H26N4O2
MW: 366.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight366.5
XLogP33.4
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count4
Rotatable Bond Count6
Exact Mass366.20557608
Monoisotopic Mass366.20557608
Topological Polar Surface Area78.7 Ų
Heavy Atom Count27
Formal Charge0
Complexity493
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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