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.
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- CAS. Nr.: 855998-67-3
- Formel: C22H30N4O5S
- Molecular Weight:462.56
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Biologische Aktivität
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 |