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Ceruletide (Caerulein) 目录号 GC30008

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1mg
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10mg
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Sample solution is provided at 25 µL, 10mM.

实验参考方法

Animal experiment:

Dogs[3]All dogs undergo serum bile acid (SBA) stimulation with food (5 kg BW 2 tablespoons) or 0.3 μg/kg BW Ceruletide IM, respectively, on consecutive days. A diet of moderate protein content and with an increased concentration of fiber is chosen to minimize metabolic complications such as hepatic encephalopathy. Before each test, the dogs are fasted for 12 hours. Blood samples are drawn at baseline, 60 and 120 minutes after feeding, and 20, 30, and 40 minutes postinjection, respectively. The blood samples are collected in plain tubes and left to clot; they are then centrifuged at 6,500 ×g for 1 minute, and the serum is used to measure SBA by a colorimetric test with endpoint determination[3].

References:

[1]. Vincent ME, et al. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34.
[2]. Bridger N, et al. Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
[3]. Steinle AU, et al. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30.
[4]. Zarrindast MR, et al. Effects of cholecystokinin receptor agonist and antagonists on morphin dependence in mice. Pharmacol Toxicol. 1995 Dec;77(6):360-4.

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Chemical Properties

Cas No. 17650-98-5 SDF Download SDF
别名 N/A
化学名 N/A
Canonical SMILES {pGlu}-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2
分子式 C58H73N13O21S2 分子量 1352.41
溶解度 H2O : ≥ 100 mg/mL (73.94 mM);DMSO : ≥ 100 mg/mL (73.94 mM) 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

Ceruletide, a biologically active decapeptide isolated from the skin of the Australian frog Hyla caerulea, is a potent cholecystokinetic agent, and acts as a cholecystokinin receptor agonist.

Ceruletide is similar chemically and biologically to the human gastrointestinal hormones cholecystokinin-pancreozymin (CCK) and gastrin II. Ceruletide stimulates gallbladder contraction, pancreatic exocrine secretion, gastric secretion, and motility in the distal duodenum, jejunum, ileum and colon, while delaying gastric emptying and inhibiting motility in the proximal duodenum[1]. Ceruletide in supramaximal but not in physiological doses activates NF-kappaB/Rel in vitro. This activation may induce a self-defending genetic program before the onset of cellular injury, which may prevent higher degrees of damage of pancreatic acinar cells after secretagogue hyperstimulation[2].

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 (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 serum bile acid (SBA) stimulation circumvents exogenous and endogenous influences associated with postprandial (PP) SBA stimulation. Ceruletide SBA stimulation may perform as well as PP SBA stimulation in dogs with portosystemic shunt (PSS) and be more sensitive for the detection of hepatic dysfunction in dogs with upper respiratory disease (URD)[3].

[1]. Vincent ME, et al. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34. [2]. Steinle AU, et al. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30. [3]. Bridger N, et al. Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8. [4]. Zarrindast MR, et al. Effects of cholecystokinin receptor agonist and antagonists on morphin dependence in mice. Pharmacol Toxicol. 1995 Dec;77(6):360-4.