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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 855998-67-3
- 分子式: C22H30N4O5S
- 分子量:462.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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 |