145084-28-2
基本信息
YM 022 >=98% (HPLC)
(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
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)-
物理化学性质
| 储存条件 | Store at RT |
| 溶解度 | DMSO：可溶，5mg/mL（澄清溶液） |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 旋光性 (optical activity) | [α]/D -128 to -140 (c = 1, DCM) |
安全数据
| 危险性符号(GHS) |  GHS06 |
| 警示词 | 危险 |
| 危险性描述 | H301 |
| 防范说明 | P301+P310 |
| 危险品标志 | T |
| 危险类别码 | 25 |
| 安全说明 | 45 |
| 危险品运输编号 | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
常见问题列表
|
CCR1 68 pM (Ki) |
CCR2 63 nM (Ki) |
YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC
50
value for [
3
H]devazepide binding of 136 nM.
YM022 inhibits the binding of [
125
I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC
50
value for [
125
I]CCK-8 binding of 0.73 nM.
Selectivity [ratio of (IC
50
for gastrin/CCK-B receptor)/(IC
50
for CCK-A receptor)] of YM022 is 186.
YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED
50
values of 0.0261 and 0.0654 μmol/kg, respectively, without affecting histamine- or methacholine-induced acid secretion.
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.
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection.
| Animal Model: | Rat |
| 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. |