1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. YM022

YM022 

Cat. No.: HY-103355 Purity: 99.00%
Handling Instructions

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.

For research use only. We do not sell to patients.

YM022 Chemical Structure

YM022 Chemical Structure

CAS No. : 145084-28-2

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10 mM * 1 mL in DMSO USD 625 Ask For Quote & Lead Time
5 mg USD 550 Ask For Quote & Lead Time

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Description

YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively[1]. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo[3].

IC50 & Target[1]

CCR1

68 pM (Ki)

CCR2

63 nM (Ki)

In Vitro

YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC50 value for [3H]devazepide binding of 136 nM[1].
YM022 inhibits the binding of [125I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC50 value for [125I]CCK-8 binding of 0.73 nM[1].
Selectivity [ratio of (IC50 for gastrin/CCK-B receptor)/(IC50for CCK-A receptor)] of YM022 is 186[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED50 values of 0.0261 and 0.0654 μmol/kg, respectively, without affecting histamine- or methacholine-induced acid secretion[3].
YM022 (subcutaneous injection; 300 μmol/kg; single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24 h after dosage). Maximum enzyme inhibition is achieved at a dose of 300 μmol/kg  for YM022 and the inhibition of HDC lasts for 4 weeks. At sacrifice, drug residues can be seen at the injection site for as long as 4 (YM022) weeks after injection in rat[3].
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat[3]
Dosage: 300 μmol/kg
Administration: Subcutaneous injection; 300 μmol/kg; single dose
Result: Suppressed the ECL cell activity for at least 4 as manifested in greatly reduced HDC activity, greatly elevated serum gastrin level.
Molecular Weight

516.59

Formula

C₃₂H₂₈N₄O₃

CAS No.

145084-28-2

SMILES

O=C(NC1=CC=CC(C)=C1)N[[email protected]]2C(N(CC(C3=CC=CC=C3C)=O)C4=CC=CC=C4C(C5=CC=CC=C5)=N2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

YM022YM 022YM-022CCRCC chemokine receptorgastric acidsecretionhistidine decarboxylaseInhibitorinhibitorinhibit

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YM022
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