Linaprazan mesylate
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.
- CAS No.: 855998-67-3
- Formula: C22H30N4O5S
- Molecular Weight:462.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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.
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 |