GIP (1-30) amide, porcine TFA is a high-affinity full agonist of the glucose-dependent insulinotropic polypeptide (GIP) receptor, having a similar potency as the native GIP(1-42) [1]. Furthermore, GIP (1-30) amide, porcine displays weak inhibitory effects on gastric acid secretion while exhibiting potent insulin-stimulating properties.
Taspoglutide是一种GLP-1受体激动剂(Taspoglutide, Ki = 1.1 nM for the human receptor),在表达该受体的CHO-K1细胞中可以诱导cAMP积累(EC50 = 0.06 nM)。在进行口服葡萄糖耐量测试的Zucker糖尿病肥胖大鼠中,每周给予Taspoglutide 1 mg 动物,结果显示其能有效降低血糖和提高胰岛素水平。此外,在相同的动物模型中,Taspoglutide还能降低胃抑制肽(GIP)和甘油三酯的血浆水平,同时减轻体重。