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  3. Linaprazan mesylate

Linaprazan mesylate  (Synonyms: AZD-0865 mesylate)

Cat. No.: HY-100412A
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Linaprazan mesylate can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid. Linaprazan (AZD0865) mesylate can be used for research on reflux esophagitis with oral activity.

For research use only. We do not sell to patients.

Linaprazan mesylate Chemical Structure

Linaprazan mesylate Chemical Structure

CAS No. : 855998-67-3

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Description

Linaprazan mesylate can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid. Linaprazan (AZD0865) mesylate can be used for research on reflux esophagitis with oral activity[1][2][3].

In Vitro

Linaprazan (AZD0865) mesylate inhibits acid formation in rabbit gastric glands stimulated by histamine or dibutyryl cAMP (IC50 values of 0.28 and 0.26 μM, respectively) [1].
Linaprazan (AZD0865) mesylate (3 μM, pH 7.4) inhibits H+, K+-ATPase activity by 88.1% [1].
Linaprazan (AZD0865) mesylate inhibits H+, K+-ATPase activity in a K+-competitive manner (Ki=46 nM) [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo


Pharmacokinetic analysis of 2.4 mg/kg Linaprazan mesylate after single oral administration in SD rats[3]

Sex t1/2 (h) Tmax (h) Cmax (ng eq./g) AUC0-t (ng·h eq./g) AUC0-∞ (ng·h eq./g) AUC% (%)
Male 5.08 4.67 455 5960 6200 4.12
Femal 4.64 4.00 1270 13900 14300 3.10

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

462.56

Formula

C22H30N4O5S

CAS No.
SMILES

O=C(C1=CN2C(C(NCC3=C(C)C=CC=C3C)=C1)=NC(C)=C2C)NCCO.CS(=O)(O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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