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Ceruletide

MCE China：Ceruletide

Brand：MedChemExpress (MCE)

Cat. No.HY-A0190

CAS：17650-98-5

Synonyms：Caerulein; Cerulein; FI-6934

Purity：99.97%

Storage：Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Ceruletide is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.

In Vitro：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].

In Vivo：Ceruletide can be used to induce pancreatitis models. When S35-labeled Ceruletide 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 Ceruletide is 1012 mg/kg[4][5]. .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of Acute Pancreatitis[6][7][8] Background Ceruletide acts on CCK receptors, which are often expressed on various species of pancreatic acinar cells. Ceruletide induces dysregulation of the production and secretion of digestive enzymes, leading to cytoplasmic vacuolization and the death of acinar cells, edema formation, and an infiltration of inflammatory cells into the pancreas. Specific Mmodeling Methods 1. Mice: C57Bl/6n mice • 8-12 week-oldAdministration: Ceruletide 50 μg/kg • i.p. • 8 hourly, total 8 times; 2. Mice: C57BL6/J mice • male • 6-8 week-old Administration: Ceruletide 100 μg/kg plus LPS (5 mg/kg, i.p. immediately after the last injection of Ceruletide) • i.p. • 10 hourly, total 10 times; or Ceruletide (50 μg/kg, 7 hourly, total 7 times) plus LPS (10 mg/kg, once) • i.p. Note (1) Cerulein induces rapid pancreatitis and rapid spontaneous recovery within one week in mammals. Therefore, mice are usually euthanized within 24 h after the first Ceruletide injection. Modeling Indicators Molecular changes: Increased serum amylase, serum lipase, TNF-α, and IL-1β level.Histology analysis: Pancreatic edema, inflammatory infiltration, and acinar cell necrosis (H&E staining). Correlated Product(s): Lipopolysaccharides(HY-D1056) Opposite Product(s): / .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of Chronic Pancreatitis[9] Background Chronic pancreatitis (CP) model can be established by repeated injection of mice with Ceruletide. Histologic characteristics of chronic pancreatitis include inflammatory infiltrates, fibrosis, acinar cell atrophy, duct distortion, and squamous metaplasia of the duct epithelium. Specific Mmodeling Methods Mice: C57BL/6 • female • 6 week-oldAdministration: Ceruletide 50 μg/kg • i.p. • 3 days per week, for a total of 4 weeks. Note Mice were sacrificed 3 days after the last injection. Modeling Indicators Histology analysis: Glandular atrophy, infiltration of immune cells and distorted and/or blocked ducts. Correlated Product(s): Pevonedistat (HY-70062) Opposite Product(s): /

Animal Administration：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].

IC50 & Target：Cholecystokinin receptor[4] In Vitro 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Ceruletide Related Antibodies

Sequence：{pGlu}-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2

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References：

[1]. Steinle AU, et al. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30.  [Content Brief]

[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.  [Content Brief]

[3]. Vincent ME, et al. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34.  [Content Brief]

[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.  [Content Brief]

[5]. Ke-You Zhang, et al. Chemically Induced Models of Pancreatitis. 2022. Pancreapedia: Exocrine Pancreas Knowledge Base, DOI: 10.3998/panc.2022.01

[6]. Wu Z, et al. Dopamine D2 Receptor Signaling Attenuates Acinar Cell Necroptosis in Acute Pancreatitis through the Cathepsin B/TFAM/ROS Pathway. Oxid Med Cell Longev. 2022 Jul 26;2022:4499219.  [Content Brief]

[7]. Kong L, et al. Sitagliptin activates the p62-Keap1-Nrf2 signalling pathway to alleviate oxidative stress and excessive autophagy in severe acute pancreatitis-related acute lung injury. Cell Death Dis. 2021 Oct 11;12(10):928.  [Content Brief]

[8]. Malla SR, et al. Early trypsin activation develops independently of autophagy in caerulein-induced pancreatitis in mice. Cell Mol Life Sci. 2020 May;77(9):1811-1825.  [Content Brief]

[9]. Lin Y, et al. Neddylation pathway alleviates chronic pancreatitis by reducing HIF1α-CCL5-dependent macrophage infiltration. Cell Death Dis. 2021 Mar 15;12(3):273.  [Content Brief]