Ceruletide 是一种十肽,是一种安全有效的胆囊收缩剂,是一种胆囊收缩素受体激动剂,对胆囊肌肉和胆管有直接的痉挛性作用。
产品描述
Ceruletide is a potent agonist of cholecystokinin receptor and it also is a safe and effective cholecystokinetic agent. It has a direct spasmogenic effect on the gallbladder muscle and bile ducts.
体外活性
Ceruletide is the same as biologically and chemically to the human gastrointestinal hormones cholecystokinin-pancreozymin (CCK) and gastrin II. Ceruletide stimulates gallbladder contraction while delaying gastric emptying and inhibiting motility in the proximal duodenum [1]. Ceruletide in supramaximal but not in physiological doses activate NF-kappaB/Rel in vitro. This activation may induce a self-defending genetic program before the onset of cellular injury and may prevent higher degrees of damage of pancreatic acinar cells after secretagogue hyperstimulation [2].
体内活性
Ceruletide (5-15 ng/kg, i.v.) shows a marked spasmogenic effect on the pylorus of rats. Ceruletide also reduces blood pressure in anesthetized dogs [1]. Ceruletide (0.4-0.5 mcg/kg, i.v.; 3-4 mcg/kg, s.c.) results in emesis and evacuation of the bowel in the intact conscious dog, and recovery is complete 15-30 min after i. v. administration and 2-4 hr after s.c. administration. Ceruletide SBA stimulation may perform as well as PP SBA stimulation in dogs with the portosystemic shunt and be more sensitive for the detection of hepatic dysfunction in dogs with the upper respiratory disease [3].
Cas No.
17650-98-5
分子式
C58H73N13O21S2
分子量
1352.41
别名
雨蛙素;Caerulein;FI-6934;Cerulein
储存和溶解度
H2O:100 mg/mL (73.94 mM)
DMSO:96 mg/mL (70.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years