YM 022A highly potent and selective non-peptide CCK-BR silent antagonist

YM 022 (CAS 145084-28-2)

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Application: A highly potent and selective non-peptide CCK-BR silent antagonist
CAS Number: 145084-28-2
Molecular Weight: 516.60
Molecular Formula: C32H28N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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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).


References

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.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (10 mM).
Storage :
Store at room temperature
Boiling Point :
~735.4° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.65 (Predicted)
Optical Activity :
α20/D -134°±6°, c = 1 in DCM
IC50 :
Cholecystokinin B receptor: IC50 = 0.11 nM (rat); Cholecystokinin A receptor: IC50 = 146 nM (rat)
Ki Data :
CCK-BR: Ki= 0.06 nM (human); CCK2: Ki= 68 pM;CCK1: Ki= 63 nM
pK Values :
pKa: 11.61 (Predicted), pKb: 2.88 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
122130
MDL Number :
MFCD00917023
SMILES :
CC1=CC(=CC=C1)NC(=O)N[C@H]2C(=O)N(C3=CC=CC=C3C(=N2)C4=CC=CC=C4)CC(=O)C5=CC=CC=C5C

Download SDS (MSDS)

Certificate of Analysis

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