Caerulein
CAS No. : 17650-98-5
(Synonyms: Ceruletide; Cerulein; FI-6934)
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| Cat. No. : | HY-A0190 |
| M.Wt: | 1352.41 |
| Formula: | C58H73N13O21S2 |
| Purity: | >98 % |
| Solubility: | H2O : 2.5 mg/mL (ultrasonic);DMSO : 100 mg/mL (ultrasonic);DMF : 16.67 mg/mL (ultrasonic) |
Caerulein is a decapeptide and a potent cholecystokinin receptor agonist. Caerulein is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts[1].
IC50 & Target:Cholecystokinin receptor[4]
In Vitro:Caerulein is similar chemically and biologically to the human gastrointestinal hormones cholecystokinin-pancreozymin (CCK) and gastrin II. Caerulein 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]. Caerulein 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].
In Vivo:Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Caerulein (0.4-0.5 μg/kg, i.v.; 3-4 μg/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. Caerulein (5-15 ng/kg, i.v.) shows a marked spasmogenic effect on the pylorus of rats. Caerulein also reduces blood pressure in anesthetized dogs[1].
Caerulein serum bile acid (SBA) stimulation circumvents exogenous and endogenous influences associated with postprandial (PP) SBA stimulation. Caerulein 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].
Caerulein can be used to induce pancreatitis models. When S35-labeled Caerulein is administered by intramuscular injection to rats, rabbits, and mice, the radioactivity in the blood of rats and rabbits reaches its peak within 5 and 15 minutes, respectively, followed by a rapid decline. Acute toxicity studies in mice show that the intravenous LD50 value for Caerulein is 1012 mg/kg[4][5]
Administration: Caerulein 50 μg/kg • i.p. • 8 hourly, total 8 times;
2. Mice: C57BL6/J mice • male • 6-8 week-old
Administration: Caerulein 100 μg/kg plus LPS (5 mg/kg, i.p. immediately after the last injection of Caerulein) • i.p. • 10 hourly, total 10 times;
or Caerulein (50 μg/kg, 7 hourly, total 7 times) plus LPS (10 mg/kg, once) • i.p.
Histology analysis: Pancreatic edema, inflammatory infiltration, and acinar cell necrosis (H&E staining).
Administration: Caerulein 50 μg/kg • i.p. • 3 days per week, for a total of 4 weeks.
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