L-168049 is a potent, selective, orally active and non-competitiveglucagon receptorantagonist withIC₅₀s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively^[1][2].

IC50: 3.7 nM (human glucagon receptor), 63 nM (murine glucagon receptor), and 60 nM (canine glucagon receptor)^[2]

L-168049 (compound 49) inhibits glucagon (100 pM) stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor (hGIAR) (IC₅₀of 41 nM). L-168049 blocks cAMP formation stimulated by glucagon in murine liver membranes^[1].
L-168049 increases the apparent EC₅₀for glucagon stimulation of adenylyl cyclase in Chinese hamster ovary cells expressing the human glucagon receptor and decreases the maximal glucagon stimulation observed, with a K_bof 25 nM^[2].

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^[3].

467.79

Solid

C₂₄H₂₀BrClN₂O

191034-25-0

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL(106.89 mM)

*"≥" means soluble, but saturation unknown.

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