Name | 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 |
Synonyms | YM-220 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]- |
CAS | 155488-25-8 |
EINECS | 604-604-1 |
Molecular Formula | C28H30N6O3 |
Molar Mass | 498.58 |
Density | 1.25 |
Boling Point | 723.0±60.0 °C(Predicted) |
pKa | 11.38±0.40(Predicted) |
Storage Condition | Room Temprature |
In vivo study | 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 . |
biological activity | Sograzepide(Netazepide; YF 476; YM-220) is a highly effective, A highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM also inhibits Gastrin/CCK-A activity with an IC50 value of 502 nM. Sograzepide(Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to rat brain, cloned canine and human Gastrin/CCK-B with Ki values of 0.068, 0.62 and 0.19 nM, respectively. |
Target | IC50: 0.1 nM (Gastrin/CCK-B); 501 nM (Gastrin/CCK-A) |