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Ceruletide

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Chemical Structure| 17650-98-5 同义名 : Cerulein;Caerulein;CCRIS-3063;FI-6934
CAS号 : 17650-98-5
货号 : A569478
分子式 : C58H73N13O21S2
纯度 : 98%
分子量 : 1352.405
MDL号 : MFCD00076478
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(77.64 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2.5 mg/mL(1.85 mM)，配合低频超声助溶

DMF: 15 mg/mL(11.09 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Cholecystokinin octapeptide (cholecystokinin-8) is found in the peripheral tissue and central nervous system (CNS). It is becoming clear that cholecystokinin-8 sulphate may function as a neurotransmitter or neuromodulator in the CNS. Thus, cholecystokinin-8 sulphate is released from synaptic vesicles in a calcium-dependent manner, binds to specific high affinity cholecystokinin receptors and exerts primarily excitatory effect on CNS neurons. One potential role that has been proposed for cholecystokinin is the modulation of central opiate nociceptive mechanism. Cholecystokinin receptors are generally divided into two classes, cholecystokinin-A (alimentary) and cholecystokin- in-B (brain)[3]. Caerulein is a decapeptide isolated from frog skin, which has been shown to possess the same biological and pharmacological activities as cholecystokinin-8[3]. Ceruletide in supramaximal but not in physiological doses activated NF-kappaB/Rel in vitro. This activation might induce a self-defending genetic program before the onset of cellular injury, which might prevent higher degrees of damage of pancreatic acinar cells after secretagogue hyperstimulation[4]. Ceruletide serum bile acid (SBA) stimulation circumvented exogenous and endogenous influences associated with postprandial (PP) SBA stimulation. Ceruletide SBA stimulation might 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)[5]. Ceruletide (0.4-0.5 mcg/kg, i.v.; 3-4 mcg/kg, s.c.) resulted in emesis and evacuation of the bowel in the intact conscious dog, and recovery was complete 15 - 30 min after i. v. administration and 2 - 4h after s.c. administration. Ceruletide (5 - 15 ng/kg, i.v.) showed a marked spasmogenic effect on the pylorus of rats. Ceruletide also reduced blood pressure in anesthetized dogs[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03748667 - Not yet recruiting December 2020 United States, California ... 展开 >> San Francisco Veterans Affairs Medical Center. University of California Not yet recruiting San Francisco, California, United States, 94121 Contact       endoresection@me.com    Principal Investigator: Tonya Kaltenbach          United States, North Carolina University of North Carolina Not yet recruiting Chapel Hill, North Carolina, United States, 27599 Contact       mcgills@email.unc.edu    Principal Investigator: Sarah McGill          Japan National Cancer Center Not yet recruiting Tokyo, Japan, 104-0045 Contact       tasakamo529@gmail.com    Principal Investigator: Taku Sakamoto          Spain Hospital Clínico Universitario Lozano Blesa Not yet recruiting Zaragoza, Aragón, Spain, 50009 Contact       angel.ferrandez@telefonica.net    Principal Investigator: Ángel Ferrández          Hospital Universitari Germans Trias i Pujol (Can Ruti) Not yet recruiting Badalona, Cataluña, Spain, 08916 Contact       hugoikuo@gmail.com    Principal Investigator: Hugo Uchima          Hospital Clínic de Barcelona Not yet recruiting Barcelona, Cataluña, Spain, 08036 Contact       MPELLISE@clinic.cat    Principal Investigator: Maria Pellisé          Sub-Investigator: Miriam Cuatrecasas          Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS) Not yet recruiting Barcelona, Cataluña, Spain, 08036 Contact       JCAMPS@clinic.cat    Sub-Investigator: Jordi Camps          Althaia. Xarxa Assistencial Universitària de Manresa Not yet recruiting Manresa, Cataluña, Spain, 08243 Contact       orosinol@althaia.cat    Sub-Investigator: Òria Rosiñol          Hospital Universitario y Politécnico de La Fe Not yet recruiting Valencia, Comunidad Valenciana, Spain, 46009 Contact       mbustamantebalen@gmail.com    Principal Investigator: Marco Bustamante          Complejo Hospitalario de Navarra Not yet recruiting Pamplona, Navarra, Spain, 31008 Contact       edualbeniz@hotmail.com    Principal Investigator: Eduardo Albéniz          Hospital Ramón y Cajal Not yet recruiting Madrid, Spain, 28034 Contact       enrodesan@gmail.com    Principal Investigator: Enrique Rodríguez          Hospital 12 de Octubre Not yet recruiting Madrid, Spain, 28041 Contact       josecarlos.marin@salud.madrid.org    Principal Investigator: José Carlos Marín 收起 <<
NCT01491178 - Completed - -
NCT02808403 - Recruiting April 30, 2022 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.74mL

0.15mL

0.07mL

3.70mL

0.74mL

0.37mL

7.39mL

1.48mL

0.74mL
参考文献

[1]Furuyama T, Tanaka S, et al. Proteasome activity is required for the initiation of precancerous pancreatic lesions. Sci Rep. 2016 May 31;6:27044.

[2]Pradel P, Estival A, et al. Caerulein and gastrin(2-17 ds) regulate differently synthesis of secretory enzymes, mRNA levels and cell proliferation in pancreatic acinar cells (AR4-2J). Biochem J. 1993 Feb 15;290 ( Pt 1):219-24.

[3]Zarrindast MR, Malekzadeh A, Rezayat M, Ghazi-Khansari M. Effects of cholecystokinin receptor agonist and antagonists on morphine dependence in mice. Pharmacol Toxicol. 1995 Dec;77(6):360-4. doi: 10.1111/j.1600-0773.1995.tb01042.x. PMID: 8835359.

[4]Steinle AU, Weidenbach H, Wagner M, Adler G, Schmid RM. NF-kappaB/Rel activation in cerulein pancreatitis. Gastroenterology. 1999 Feb;116(2):420-30. doi: 10.1016/s0016-5085(99)70140-x. PMID: 9922324.

[5]Bridger N, Glanemann B, Neiger R. Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8. doi: 10.1111/j.1939-1676.2008.0114.x. PMID: 18537882.

[6]Vincent ME, Wetzner SM, Robbins AH. Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34. doi: 10.1002/j.1875-9114.1982.tb03189.x. PMID: 6763205.