This GIP fragment has potent insulinotropic activity in the isolated, perfused rat pancreas but greatly reduced somatostatinotropic activity in the isolated perfused rat stomach. The site responsible for insulinotropic activity apparently lies between residues 19 and 30 of GIP.
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。