155488-25-8

中文名称 N-[(3R)-1-(3,3-Dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea

英文名称 N-[(3R)-1-(3,3-Dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea

CAS 155488-25-8

分子式 C28H30N6O3

分子量 498.58

MOL 文件 155488-25-8.mol

155488-25-8 结构式

基本信息物理化学性质 N-[(3R)-1-(3,3-Dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea价格(试剂级) 常见问题列表

基本信息

中文别名

N-[(3R)-1-(3,3-二甲基-2-氧代丁基)-2,3-二氢-2-氧代-5-(2-吡啶基)-1H-1,4-苯并二氮杂卓-3-基]-N'-[3-(甲基氨基)苯基]脲

英文别名

Sograzepide
Estradiol-3-O-sulfamate
1-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl]-3-[3-(methylamino)phenyl]urea
N-[(3R)-1-(3,3-Dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea
Urea, N-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]-

物理化学性质

沸点723.0±60.0 °C(Predicted)

密度1.25

储存条件-20°C储存

溶解度DMSO : ≥ 100 mg/mL (200.57 mM)

酸度系数(pKa)11.38±0.40(Predicted)

形态Solid

颜色Off-white to light yellow

常见问题列表

生物活性

Sograzepide (Netazepide; YF 476; YM-220) 是一种非常有效，高选择性和口服活性的 Gastrin/CCK-B 拮抗剂，IC50 值为 0.1 nM，还抑制 Gastrin/CCK-A 活性， IC50 值为 502 nM。Sograzepide (Netazepide; YF 476; YM-220) 取代 [125I]CCK-8 与大鼠脑，克隆犬和人 Gastrin/CCK-B 的特异性结合，Ki 值分别为 0.068、0.62 和 0.19 nM。

靶点

IC50: 0.1 nM (Gastrin/CCK-B); 501 nM (Gastrin/CCK-A)

体内研究

Sograzepide (Netazepide; YF 476; YM-220) (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anethsetized rats with an ED ₅₀ of 87 nmol/kg. Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion with an ED ₅₀ value of 0.0086 μM/kg, but does not affect histamine- and bethanechol-induced acid secretion.Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; oral administration) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner with ED ₅₀ values of 0.018 and 0.020 μM/kg, respectively .