[CAS NO. 248919-64-4] Linaprazan
PRODUCTS SPECIFICATIONS [248919-64-4]
DESCRIPTION [248919-64-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 366.46 |
| Molecular Formula | C21H26N4O2 |
| SMILES | O=C(C1=CN2C(C(NCC3=C(C)C=CC=C3C)=C1)=NC(C)=C2C)NCCO |
Summary
Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition. In vitro: Linaprazan can inhibit the final step in acid secretion. Linaprazanreduced porcine renal Na+,K+-ATPase activity by 9 ± 2%, demonstrating a high selectivity for H+,K+-ATPase. In vivo: The reference for animal administration is 0.5-1.0 mg/kg. The greater degree of acid suppression with the 75-mg dose of Linaprazan would translate to a healing rate of 89% at 4 weeks.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00206284 | AstraZeneca |
GERD Without Erosive Esophagitis
|
May 2004 | Phase 2 |
| NCT00206245 | AstraZeneca |
GERD With Erosive Esophagitis
|
May 2004 | Phase 2 |
| NCT05469854 | Cinclus Pharma AG |
Pharmacokinetics|Cardiodynamic ECG|Safety, and Tolerability|GERD
|
July 13, 2022 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 35 mg/mL ( 95.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7288 mL | 13.6441 mL | 27.2881 mL |
| 5 mM | 0.5458 mL | 2.7288 mL | 5.4576 mL |
| 10 mM | 0.2729 mL | 1.3644 mL | 2.7288 mL |
References
- [1] Gedda K et al. Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+,K+-ATPase. Biochem Pharmacol. 2007 Jan 15;73(2):198-205.
- [2] Kahrilas PJ et al. A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis. Clin Gastroenterol Hepatol. 2007 Dec;5(12):1385-91.
