Exendin-4

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Chemical Structure| 141758-74-9 同义名 : 艾塞那肽-4 ;Exenatide
CAS号 : 141758-74-9
货号 : A561110
分子式 : C184H282N50O60S
纯度 : 98%
分子量 : 4186.57
MDL号 : MFCD00240171
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(7.17 mM)，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: 30 mg/mL(7.17 mM)，配合低频超声助溶
生物活性
描述 Glucagon-like peptide-1 (GLP-1) is an enteroendocrine hormone that has a capacity, when administered exogenously, to normalize blood glucose levels in type 2 diabetes mellitus. Exendin-4, a 39-amino acid (AA) peptide, is a long-acting agonist at the GLP-1 receptor with an IC50 value of 3.22 nM[3]. In human umbilical vein endothelial cells (HUVECs), exendin-4 significantly increased NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner[4]. In vivo, ob/ob mice sustained a reduction in the net weight gained during exendin-4 treatment (10 μg/kg or 20 μg/kg for 60 days). Furthermore, serum glucose and hepatic steatosis was significantly reduced and insulin sensitivity was improved in exendin-4 treated ob/ob mice[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.24mL

0.05mL

0.02mL

1.19mL

0.24mL

0.12mL

2.39mL

0.48mL

0.24mL
参考文献

[1]Tsutsumi Y, Nomiyama T, et al. Combined Treatment with Exendin-4 and Metformin Attenuates Prostate Cancer Growth. PLoS One. 2015 Oct 6;10(10):e0139709.

[2]Zhou Y, He X, et al. Exendin-4 attenuates cardiac hypertrophy via AMPK/mTOR signaling pathway activation. Biochem Biophys Res Commun. 2015 Dec 4-11;468(1-2):394-9.

[3]Doyle ME, Theodorakis MJ, et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and for biological activity. Regul Pept. 2003 Jul 15;114(2-3):153-8

[4]Wei R, Ma S, Wang C, 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

[5]Ding X, Saxena NK, Lin S, Gupta NA, Anania FA. Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/ob mice. Hepatology. 2006 Jan;43(1):173-81