CCK-B Receptor Antagonist 2

Names

[ Name ]:
CCK-B Receptor Antagonist 2

Biological Activity

[Description]:

CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC50 of 1.82 μM[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor

Research Areas >> Metabolic Disease

[Target]

IC50: 0.43 nM (Gastrin/CCK-B); 1.82 μM (Gastrin/CCK-A)[1]

[In Vivo]

CCK-B Receptor Antagonist 2 (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anethsetized rats with an ED50 of 8.3 nmol/kg[1].

[References]

[1]. Semple G, et al. (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.J Med Chem. 1997 Jan 31;40(3):331-41.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₂₈N₆O₃

[ Molecular Weight ]:
484.55

Related Compounds

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