Ceruletide-Caerulein-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECeruletideCat. No.: HY-A0190CAS No.: 17650-98-5Synonyms: Caerulein; Cerulein; FI-6934分式: CHNOS分量: 1352.41Sequence: pGlu-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2Sequence Shortening: pGlu-QD-Y(SO3H)-TGWMDF-NH2作靶点: Cholecystok

2、inin Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Protect from lightPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 H2O : 100 mg/mL (73.94 mM)DMSO : 100 mg/mL (73.94 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Con

3、centration制备储备液1 mM 0.7394 mL 3.6971 mL 7.3942 mL5 mM 0.1479 mL 0.7394 mL 1.4788 mL10 mM 0.0739 mL 0.3697 mL 0.7394 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根

4、据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (1.54 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (1.54 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (1.

5、54 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Ceruletide (Caerulein)从澳利亚 蛙肤中分离的物活性肽，种有效的胆囊收缩剂，为缩胆囊素受体 (cholecystokinin receptor) 激动剂。IC50 & Target Cholecystokinin receptor 4体外研究 Ceruletide is similar chemically and biologically to the human gastrointestinal hormones cholecystokinin-panc

6、reozymin (CCK) and gastrin II. Ceruletide stimulates gallbladder contraction, pancreatic exocrinesecretion, gastric secretion, and motility in the distal duodenum, jejunum, ileum and colon, while delayinggastric emptying and inhibiting motility in the proximal duodenum 1. Ceruletide in supramaximal

7、but not inphysiological doses activates NF-kappaB/Rel in vitro. This activation may induce a self-defending geneticprogram before the onset of cellular injury, which may prevent higher degrees of damage of pancreatic acinarcells after secretagogue hyperstimulation 2.体内研究 Ceruletide (0.4-0.5 mcg/kg,

8、i.v.; 3-4 mcg/kg, s.c.) results in emesis and evacuation of the bowel in the intactconscious 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

9、reduces blood pressure in anesthetized dogs 1. Ceruletide serum bile acid (SBA)stimulation circumvents exogenous and endogenous influences associated with postprandial (PP) SBAstimulation. Ceruletide SBA stimulation may perform as well as PP SBA stimulation in dogs withportosystemic shunt (PSS) and

10、be more sensitive for the detection of hepatic dysfunction in dogs with upperrespiratory disease (URD) 3.PROTOCOLAnimal Dogs 3Administration 3 All dogs undergo serum bile acid (SBA) stimulation with food (5 kg BW 2 tablespoons) or 0.3 g/kg BWCeruletide IM, respectively, on consecutive days. A diet o

11、f moderate protein content and with an increasedconcentration of fiber is chosen to minimize metabolic complications such as hepatic encephalopathy. Beforeeach test, the dogs are fasted for 12 hours. Blood samples are drawn at baseline, 60 and 120 minutes afterfeeding, and 20, 30, and 40 minutes pos

12、tinjection, respectively. The blood samples are collected in plaintubes and left to clot; they are then centrifuged at 6,500 g for 1 minute, and the serum is used to measure2/3 Master of Small Molecules 您边的抑制剂师www.MedChemESBA by a colorimetric test with endpoint determination 3.MCE has not independe

13、ntly confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Biochem Pharmacol. 2019 Mar;161:149-162. Front Immunol. 2019 May 3;10:980. J Cell Physiol. 2019 May 6. Am J Transl Res. 2018 Feb 15;10(2):402-410. Mol Immunol. 2018 Nov;103:78-88.See more customer validations on HY

14、PERLINK / www.MedChemEREFERENCES1. 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 Toxico