1. GPCR/G Protein
  2. Glucagon Receptor
  3. L-168049

L-168049 

Cat. No.: HY-103547
Handling Instructions

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

For research use only. We do not sell to patients.

L-168049 Chemical Structure

L-168049 Chemical Structure

CAS No. : 191034-25-0

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Description

L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively[1][2].

IC50 & Target

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

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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

467.79

Formula

C₂₄H₂₀BrClN₂O

CAS No.
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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L-168049
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