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作靶點(diǎn): Cholecystok

2、inin Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Protect from lightPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根

4、據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (1.54 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (1.54 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (1.

5、54 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Ceruletide (Caerulein)從澳利亞 蛙膚中分離的物活性肽，種有效的膽囊收縮劑，為縮膽囊素受體 (cholecystokinin receptor) 激動(dòng)劑。IC50 & Target Cholecystokinin receptor 4體外研究 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.體內(nèi)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 您邊的抑制劑師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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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