名称 | Exendin-4 |
描述 | Exendin-4 (Exenatide) 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]. |
存储条件 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 10 mM H2O : 1.23 mg/mL, Sonication and heating are recommended.
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关键字 | inhibit | GCGR | Inhibitor | Exendin-4 | 141732-76-5 | Exendin 4 | Glucagon Receptor | Exendin4 |
相关产品 | Tirzepatide Acetate(2023788-19-2 free base) | PF-06882961 Tris | PF-06882961 | Glucagon (1-29), bovine, human, porcine hydrochloride | (S, R)-LSN 3318839 | NNC 92-1687 | Adomeglivant | 6α-Methylprednisolone 21-hemisuccinate sodium salt | Orforglipron | LSN3318839 |
相关库 | ReFRAME 相关化合物库 | NO PAINS 化合物库 |