Exendin-4-Acetate-Exenatide-acetate-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEExendin-4 AcetateCat. No.: HY-13443ACAS No.: 914454-01-6Synonyms: Exenatide acetate分式: CHNOS分量: 4246.62Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly

2、-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2Sequence Shortening: HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2作靶點: Glucagon Receptor作通路: GPCR/G Protein儲存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 66.66 mg/mL (15.70 mM)H2O : 0.1 mg/mL (insoluble)* means solubl

3、e, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 0.2355 mL 1.1774 mL 2.3548 mL5 mM 0.0471 mL 0.2355 mL 0.4710 mL10 mM 0.0235 mL 0.1177 mL 0.2355 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Exendin-4

4、 Acetate是由39個氨基酸組成的多肽。它是長效的glucagon-like peptide-1受體激動劑，IC50值為3.22 nM。IC50 & Target IC50: 3.22 nM (glucagon-like peptide-1 receptor) 1體外研究 In human umbilical vein endothelial cells, Exendin-4 significantly increases NO production, endothelial NOsynthase (eNOS) phosphorylation, and GTP cyclohydrolase

5、 1 (GTPCH1) level in a dose-dependent manner2. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 M at 48 hour 3.體內(nèi)研究 Both low- and high-dose Exendin-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose,and calculated HOMA scores compared with control. Exen

6、din-4-treated ob/ob mice sustain a markedreduction in the net weight gain in the final 4 weeks of the study period 4. Animals treated with Exendin-4have more pancreatic acinar inflammation, more pyknotic nuclei and weigh significantly less than control rats.Exendin-4 treatment is associated with low

7、er leptin levels as well as lower HOMA values in rats 5.Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptorand is mediated mainly by H2S but also by NO and CO 6.PROTOCOLAnimal Rats: 20 Sprague-Dawley male rats, ten of which are treated with exendi

8、n-4 (10 g/kg) and ten of which areAdministration 45 used as controls. The study period is 75 days. Serum and pancreatic tissue are removed for biochemical andhistological study. Blood glucose, amylase, lipase and adipocytokines are compared between the two groups5.Mice: The exendin-4 treatment group

9、s are treated with 10 g/kg every 24 hours for the first 14 days. Thistreatment is the induction phase. Respective control mice (lean and ob/ob) receive saline every 24 hours.After 14 days Exendin-4-treated mice are randomly divided into two groups: one group receives high doseexendin-4 (20 g/kg) eve

10、ry 12 hours, while the second group continues with low dose exendin-4 (10 g/kg)every 12 hours. The control mice continue to receive saline every 12 hours. The mice are weighed daily forthe 60-day treatment period 4.MCE has not independently confirmed the accuracy of these methods. They are for refer

11、ence only.戶使本產(chǎn)品發(fā)表的科研獻 J Biol Chem. 2018 Nov 23;293(47):18086-18098. Sci Rep. 2017 Jun 28;7(1):4351. Neurogastroenterol Motil. 2019 Feb;31(2):e13482. Chem Biol Interact. 2019 May 1;304:186-193. Acta Biochim Biophys Sin (Shanghai). 2017 Jul 1;49(7):573-580.See more customer validations on HYPERLINK /

12、www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Doyle ME, et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and forbiological activity. Regul Pept. 2003 Jul 15;114(2-3):153-8.2. Wei R, et al. Exenatide exerts dir

13、ect protective effects on endothelial cells through the AMPK/Akt/eNOS pathway in a GLP-1 receptor-dependent manner. Am J Physiol Endocrinol Metab. 2016 Jun 1;310(11):E947-57.3. Fidan-YaylalI G, et al. Antidiabetic exendin-4 activates apoptotic pathway and inhibits growth of breast cancer cells. Tumo

14、ur Biol. 2016Feb;37(2):2647-53.4. Ding X, et al. Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/obmice. Hepatology. 2006Jan;43(1):173-81.5. Nachnani JS, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010 Jan;53(1):153-9.6. Slley E, et al. Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production.Cardiovasc Diabetol.