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155488-25-8

中文名稱 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
英文名稱 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 結(jié)構(gòu)式 155488-25-8 結(jié)構(gòu)式

基本信息

中文別名
N-[(3R)-1-(3,3-二甲基-2-氧代丁基)-2,3-二氫-2-氧代-5-(2-吡啶基)-1H-1,4-苯并二氮雜卓-3-基]-N'-[3-(甲基氨基)苯基]脲
英文別名
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]-

物理化學性質(zhì)

沸點723.0±60.0 °C(Predicted)
密度1.25
儲存條件-20°C儲存
溶解度DMSO : ≥ 100 mg/mL (200.57 mM)
酸度系數(shù)(pKa)11.38±0.40(Predicted)
形態(tài)Solid
顏色Off-white to light yellow

常見問題列表

生物活性
Sograzepide?(Netazepide; YF 476; YM-220) 是一種非常有效，高選擇性和口服活性的 Gastrin/CCK-B 拮抗劑，IC50 值為 0.1 nM，還抑制 Gastrin/CCK-A 活性， IC50 值 為 502 nM。Sograzepide?(Netazepide; YF 476; YM-220) 取代 [125I]CCK-8 與大鼠腦，克隆犬和人 Gastrin/CCK-B 的特異性結(jié)合，Ki 值分別為 0.068、0.62 和 0.19 nM。
靶點

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

體內(nèi)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 .

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