Sograzepide

Sograzepide?(Netazepide; YF 476; YM-220) is an extremely?potent?, highly?selective?and orally active Gastrin/CCK-B antagonist with an IC₅₀ value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC₅₀ of 502 nM^[1]. Sograzepide?(Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human?Gastrin/CCK-B receptors, with K_i values of 0.068, 0.62 and 0.19 nM, respectively^[2]. IC50 & Target: IC50: 0.1 nM (Gastrin/CCK-B); 501 nM (Gastrin/CCK-A)^[1] In Vivo: Sograzepide?(Netazepide; YF 476; YM-220) (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anethsetized rats with an ED₅₀ of 87?nmol/kg^[1].
Sograzepide?(Netazepide; YF 476; YM-220) (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion with an ED₅₀ value of 0.0086 μM/kg, but does not affect histamine- and bethanechol-induced acid secretion^[2].
Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; oral administration) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner with ED₅₀ values of 0.018 and 0.020 μM/kg, respectively ^[2].