Exendin-4 (Synonyms: 艾塞那肽; Exenatide)
分子量：4186.57
Formula：C184H282N50O60S
CAS 號(hào)：141758-74-9
產(chǎn)品描述：Exendin-4 (Exenatide) 是由 39 個(gè)氨基酸組成的多肽。它是長效的 glucagon-like peptide-1 受體激動(dòng)劑，IC50 值為 3.22 nM。
單字母：HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2
三字母：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-Gly-Ala-Pro-Pro-Pro-Ser-NH2
體外研究：
In human umbilical vein endothelial cells, exendin-4 significantly increases NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 μM at 48 hour.
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. Exendin-4-treated ob/ob mice sustain a marked reduction in the net weight gain in the final 4 weeks of the study period. Animals treated with exendin-4 have more pancreatic acinar 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. Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by NO and CO.
