YM 022 is a highly potent and selective non-peptide CCK-BR silent antagonist (Ki values are 68 pM and 63 nM at CCK-BR and CCK-AR, respectively).
Nishida et al (1994) Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. J.Pharmacol.Exp.Ther. 269 725. Beinborn et al (1998) Small synthetic ligands of the cholecystokinin-B/gastrin receptor can mimic the function of endogenous peptide hormones. Yale J.Biol.Med. 71 337. Kitano et al (2000) Long-lasting cholecystokinin2 receptor blockade after a single subcutaneous injection of YF476 or YM022. Br.J.Pharmacol. 130 699.
Soluble in DMSO (100 mM), and ethanol (10 mM).
Store at room temperature
~735.4° C at 760 mmHg (Predicted)
~1.2 g/cm3 (Predicted)
n20D 1.65 (Predicted)
α20/D -134°±6°, c = 1 in DCM
Cholecystokinin B receptor: IC50 = 0.11 nM (rat); Cholecystokinin A receptor: IC50 = 146 nM (rat)
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