145084-28-2
145084-28-2 structure
- Name: YM 022
- Chemical Name: YM 022,(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
- CAS Number: 145084-28-2
- Molecular Formula: C32H28N4O3
- Molecular Weight: 516.59000
- Catalog: Signaling Pathways GPCR/G Protein CCR
- Create Date: 2016-03-17 02:27:46
- Modify Date: 2024-01-09 10:33:09
-
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].
| Name | YM 022,(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 | ym 022 |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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]. |
| 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. |
| References |
| Density | 1.23g/cm3 |
|---|---|
| Boiling Point | 735.4ºC at 760mmHg |
| Melting Point | 187-190 °C |
| Molecular Formula | C32H28N4O3 |
| Molecular Weight | 516.59000 |
| Flash Point | 398.6ºC |
| Exact Mass | 516.21600 |
| PSA | 90.87000 |
| LogP | 5.48260 |
| Vapour Pressure | 1.72E-21mmHg at 25°C |
| Index of Refraction | 1.647 |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| Hazard Codes | T+ |
| RIDADR | UN 2811 6.1 / PGIII |