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Sograzepide (Netazepide) is an orally active, selective and highly potent gastrin/CCK-B antagonist that inhibits gastrin/CCK-A activity and pappalysin 2 expression in type 1 gastric neuroendocrine tumors, and can induce regression of type 1 gastric neuroendocrine tumors.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $84 | In Stock | |
5 mg | $358 | In Stock |
Description | Sograzepide (Netazepide) is an orally active, selective and highly potent gastrin/CCK-B antagonist that inhibits gastrin/CCK-A activity and pappalysin 2 expression in type 1 gastric neuroendocrine tumors, and can induce regression of type 1 gastric neuroendocrine tumors. |
Targets&IC50 | Gastrin/CCK-A:501 nM, Gastrin/CCK-B:0.1 nM |
In vivo | Intravenous Sograzepide (0.1 μmol/kg) inhibited gastrin-induced gastric acid secretion in anesthetized rats at a dose of ED50 = 87 nM/kg. [1] At a dose of 10 μM/kg, Sograzepide showed inhibition of gastrin-induced gastric acid secretion with an ED50 = 0.0086 μM/kg, but had no effect on histamine- and bethanechol-induced gastric acid secretion. [2] |
Alias | YM-220, YM220, YF476, YF 476, Netazepide |
Molecular Weight | 498.58 |
Formula | C28H30N6O3 |
Cas No. | 155488-25-8 |
Smiles | C(C(C(C)(C)C)=O)N1C=2C(C(=N[C@@H](NC(NC3=CC(NC)=CC=C3)=O)C1=O)C4=CC=CC=N4)=CC=CC2 |
Relative Density. | 1.25 g/cm3 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL(160.46 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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