L-168049 是一种选择性和非竞争性人胰高血糖素受体拮抗剂，对人、鼠和犬的 IC50 分别为 3.7 nM、63 nM 和 60 nM。

L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.

In Chinese hamster ovary cells expressing the human glucagon receptor, L-168049 increases the apparent EC50 of glucagon-stimulated adenylate cyclase and decreases maximal glucagon stimulation with a Kb of 25 nM[1]. L-168049 blocks glucagon-stimulated cAMP formation in mouse liver membrane and inhibits glucagon (100 pM)-stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor with IC50 of 41 nM [3].

In the liver of L-G6pc-/- mice, L-168049 (50 mg/kg body; p.o.) reduces Pck1 mRNA expression by half within 6 hours. L-168049 prevents the increase in G6pc expression in the kidney and gut [2].

191034-25-0

C24H20BrClN2O

467.79

L-168,049

DMSO:45mg/mL (96.2mM)
Ethanol:<46.78mg/ml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years