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Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Target：CCK-2 in vitro: Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. Check for active clinical trials or closed clinical trials using this agent. in vivo: Z-360 is a novel orally active CCK-2/gastrin receptor antagonist, significantly inhibits the growth of subcutaneous xenografts of human pancreatic tumor cells in mice, and that Z-360 combined with gemcitabine prolonged survival in a pancreatic carcinoma orthotopic xenograft mice.
| Molecular Weight | 520.62 |
| Formula | C29H36N4O5 |
| CAS Number | 209219-38-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 32 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Cholecystokinin Receptor Products |
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| Pentagastrin
Pentagastrin (ICI-50123) is a synthetic polypeptide that has effects like gastrin when given parenterally. |
| Proglumide sodium salt
Proglumide sodium salt is a non-selective, orally active cholecystokinin (CCK) antagonist. |
| Lintitript
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). |
| Lorglumide sodium salt
Lorglumide (CR-1409) sodium salt is a potent cholecystokinin (CCK) receptor antagonist. |
| Gastrin-I (human)
Gastrin-I (human) is the endogenous peptide produced in the stomach, which increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor. |
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