Exenatide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Exenatide (Exendin-4) 是一种 39 个氨基酸肽，高效、长效胰高血糖素样肽-1 受体 (GLP-1) 激动剂，IC50 为 3.22 nM。

Exenatide (Exendin-4) is a 39-aa peptide, highly potent, long-acting glucagon-like peptide-1 receptor (GLP-1) agonist with IC50 of 3.22 nM; significantly increases NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner in human umbilical vein endothelial cells, exhibits cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 uM; reduces serum glucose, insulin levels and calculated HOMA in ob/ob mice.Diabetes Phase 3 Clinical(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.

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.

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.

Exendin-4

GPCR/G Protein

Glucagon Receptor

glucagon-likepeptide-1receptor

Metabolic Disease

Diabetes

141758-74-9

4186.572

C184H282N50O60S

>98% (HPLC)

DMSO: ≥ 32 mg/mL; H2O: 1.23 mg/mL (Need ultrasonic and warming)

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L-Serinamide, L-histidylglycyl-L-a-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-a-aspartyl-L-leucyl-L-seryl-L-lysyl-L-glutaminyl-L-methionyl-L-a-glutamyl-L-a-glutamyl-L-a-glutamyl-L-alanyl-L-valyl-L-arginyl-L-leucyl-L-phenylalanyl-L-isole

(-20℃)

With Ice Pack

≥ 2 years