Sograzepide is an effective and highly selective Gastrin/CCK-B antagonist (IC50: 0.1 nM), has an inhibitory effect on Gastrin/CCK-A activity (IC50: 502 nM). Sograzepide replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine, and cloned human Gastrin/CCK-B receptors (Ki: 0.068, 0.62 and 0.19 nM, respectively).

Sograzepide (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anesthetized rats (ED50: 87?nmol/kg). Sograzepide (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion (ED50: 0.0086 μM/kg). Sograzepide (intravenous injection; p.o.) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner (ED50: 0.018 and 0.020 μM/kg, respectively) [1][2].

155488-25-8

C28H30N6O3

498.58

YF 476;Netazepide;YM-220

DMSO:100 mg/mL (200.57 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years