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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEExendin-4Cat. No.: HY-13443CAS No.: 141758-74-9Synonyms: Exenatide分式: CHNOS分量: 4186.57Sequence: 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-Gly-Pro-Ser-Ser-
2、Gly-Ala-Pro-Pro-Pro-Ser-NH2Sequence Shortening: HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2作靶点: Glucagon Receptor作通路: GPCR/G Protein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 DMSO : 32 mg/mL (7.64 mM)H2O : 1.23 mg/mL (0
3、.29 mM; Need ultrasonic and warming)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.2389 mL 1.1943 mL 2.3886 mL5 mM 0.0478 mL 0.2389 mL 0.4777 mL10 mM - - -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。1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体内实验 请
4、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(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: 2.5 mg/mL (0.60 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (0.6
5、0 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (0.60 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Exendin-4是由39个氨基酸组成的多肽。它是长效的glucagon-like peptide-1受体激动剂,IC50值为3.22nM。IC50 & Target IC50: 3.22 nM (glucagon-like peptide-1 receptor) 1体外研究 In human umbilical vein endothelial
6、 cells, exendin-4 significantly increases NO production, endothelial NOsynthase (eNOS) phosphorylation, and GTP cyclohydrolase 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.体内研究 Both low- and high-dose exend
7、in-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose,and calculated HOMA scores compared with control. Exendin-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 acina
8、r inflammation, more pyknotic nuclei and weigh significantly less than control rats.Exendin-4 treatment is associated with lower 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 mediate
9、d mainly by H2S but also by NO and CO 6.PROTOCOLAnimal Rats: 20 Sprague-Dawley male rats, ten of which are treated with exendin-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 stu
10、dy. Blood glucose, amylase, lipase and adipocytokines are compared between the two groups5.Mice: The exendin-4 treatment groups 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.
11、After 14 days Exendin-4-treated mice are randomly divided into two groups: one group receives high doseexendin-4 (20 g/kg) every 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 weighe
12、d daily forthe 60-day treatment period 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 J Biol Chem. 2018 Nov 23;293(47):18086-18098. Sci Rep. 2017 Jun 28;7(1):4351. Neurogastroenterol Motil.
13、 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 / www.MedChemEREFERENCES1. Doyle ME, et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding
14、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 direct 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.
15、3. Fidan-YaylalI G, et al. Antidiabetic exendin-4 activates apoptotic pathway and inhibits growth of breast cancer cells. Tumour 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. Selley E, et al. Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production
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