产品
编 号:F184798
分子式:C28H30N6O3
分子量:498.58
产品类型
结构图
CAS No: 155488-25-8
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产品详情
生物活性:
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. 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 Ki values of 0.068, 0.62 and 0.19 nM, respectively.
体内研究:
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.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.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 .