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Exendin-4

CAS No. : 141758-74-9

MCE 国际站：Exendin-4

产品活性：Exendin-4 (Exenatide) 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 3.22 nM。

研究领域：GPCR/G Protein

作用靶点：GCGR

In Vitro: 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.

In Vivo: 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.

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