Exendin-4 是一种长效的glucagon-likepeptide-1 受体激动剂(IC50: 3.22 nM),是一种由 39 个氨基酸组成的多肽。
产品描述
Exendin-4 is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.
体外活性
In HUVECs, exendin-4 dose-dependently significantly increases NO production, eNOS phosphorylation and GTPCH1 level[2]. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells (IC50 5 μM) at 48 hours [3].
体内活性
In ob/ob mice, the treatment of exendin-4 improve serum ALT and reduce serum glucose, insulin levels and calculated HOMA scores compared with control. In the final 4 weeks of the study period, exendin-4-treated ob/ob mice sustain an obvious reduction in the net weight gain[4]. Animals treated with exendin-4 have more pyknotic nuclei, more pancreatic acinar inflammation and weigh significantly less than control rats[5]. Exenatide leads to dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by CO and NO[6].
Cas No.
141758-74-9
分子式
C184H282N50O60S
分子量
4186.57
别名
Exenatide;艾塞那肽;Exenatide Acetate
储存和溶解度
DMSO:10 mM
H2O:1.23 mg/mL),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years