(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA
(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA Basic information
- Product Name:
- (R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA
- Synonyms:
-
- (R)-N-(2,3-Dihydro-1-(2-(2-methylphenyl)-2-oxoethyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-N'-(3-methylphenyl)urea
- (R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA
- YM 022
- N-[(3R)-2,3-Dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea
- Urea, N-[(3R)-2,3-dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)-
- YM 022 >=98% (HPLC)
- YM022,YM-022
- CAS:
- 145084-28-2
- MF:
- C32H28N4O3
- MW:
- 516.59
- Product Categories:
-
- Cholecystokinin (CCK) receptor
- Mol File:
- 145084-28-2.mol
(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA Chemical Properties
- Melting point:
- 187-190 °C
- Boiling point:
- 735.4±60.0 °C(Predicted)
- Density
- 1.23±0.1 g/cm3(Predicted)
- storage temp.
- Store at RT
- solubility
- DMSO: soluble5mg/mL (clear solution)
- form
- powder
- pka
- 11.61±0.40(Predicted)
- color
- white to beige
- optical activity
- [α]/D -128 to -140 (c = 1, DCM)
(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA Usage And Synthesis
Uses
YM 022, is a potent, selective non-peptide antagonist of the gastrin/cholecystokinin (CCK)-B receptor. (Ki values are 68 pM and 63 nM at CCK2 and CCK1 receptors respectively).
Biological Activity
Extremely potent and highly selective non-peptide CCK 2 silent antagonist (K i values are 68 pM and 63 nM at CCK 2 and CCK 1 receptors respectively). Acts in vivo to potently inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation with a long duration of action.
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].
| 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. |
IC 50
CCR2: 68 pM (Ki); CCR1: 63 nM (Ki)
storage
Store at RT
(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREASupplier
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(R)-N-[2,3-DIHYDRO-1-[2-(2-METHYLPHENYL)-2-OXOETHYL]-2-OXO-5-PHENYL-1H-1,4-BENZODIAZEPIN-3-YL]-N'-(3-METHYLPHENYL)-UREA(145084-28-2)Related Product Information
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