Linaprazan
CAS No. : 248919-64-4
(Synonyms: AZD0865)
| Size | Price | Stock |
|---|---|---|
| 5mg | $90 | In-stock |
| 10mg | $150 | In-stock |
| 25mg | $300 | In-stock |
| 50mg | $450 | In-stock |
| 100mg | $700 | In-stock |
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| Cat. No. : | HY-100412 |
| M.Wt: | 366.46 |
| Formula: | C21H26N4O2 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 35 mg/mL |
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].
In Vitro:Linaprazan (AZD0865) 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].
In Vivo:
Pharmacokinetic analysis of 2.4 mg/kg Linaprazan 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 |