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CAS No. : 191034-25-0
MCE 国际站:L-168049
产品活性:L-168049 是一种有效的、选择性的、具有口服活性的非竞争性胰高血糖素受体 (glucagon receptor) 拮抗剂,对人、鼠和犬胰高血糖素受体的 IC50 分别为 3.7 nM,63 nM 和 60 nM。
研究领域:GPCR/G Protein
作用靶点:GCGR
In Vitro: L-168049 (compound 49) inhibits glucagon (100 pM) stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor (hGIAR) (IC50 of 41 nM). L-168049 blocks cAMP formation stimulated by glucagon in murine liver membranes.
L-168049 increases the apparent EC50 for glucagon stimulation of adenylyl cyclase in Chinese hamster ovary cells expressing the human glucagon receptor and decreases the maximal glucagon stimulation observed, with a Kb of 25 nM.
In Vivo: In the liver of L-G6pc−/- mice, Pck1 mRNA expression is decreased by half 6 h after the administration of L-168049 (50 mg/kg body; p.o.), demonstrating the efficiency of the suppression of glucagon signaling. In agreement with the role of glucagon in the induction of extrahepatic gluconeogenesis, the administration of the L-168049 prevents the increase of the G6pc expression in both the kidneys and intestine of 6 h-fasted L-G6pc−/- mice.
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