产品
编 号:F302212
分子式:C152H232N40O45
分子量:3339.71
产品类型
结构图
CAS No: 275371-94-3
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产品详情
生物活性:
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM.
体内研究:
Taspoglutide has been shown to enhance the rate of glucose-induced insulin secretion from isolated, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide in Sprague-Dawley rats and diabetic db/db mice have shown a dose-related enhancement of glucose-dependent insulin release, which lower blood glucose in the db/db mouse model of type 2 diabetes. Acute treatment with taspoglutide reduces glucose excursion and increased insulin response during oGTT. In chronically treated rats, glucose excursion and levels of GIP, PYY and triglycerides during oGTT on day 21 are significantly reduced. Hepatic triglyceride levels are significantly reduced in livers from taspoglutide-treated. Taspoglutide does not reduce plaque area or lipid content in the aortic arch or abdominal aorta, and no significant change in aortic macrophage accumulation is detected after taspoglutide or metformin mice.
体外研究:
Taspoglutide (R1583/BIM51077) is a long acting 10% formulation of (Aib8-35) human GLP-1 (7-36 amides) with 93% homology with the native polypeptide. It activates the GLP-1 receptor. Taspoglutide has comparable affinity (affinity constant 1.1±0.2 nM) to the natural ligand (affinity constant 1.5±0.3 nM) for the hGLP-1 receptor and exhibits comparable potency in stimulating cAMP production.