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L-168049

Catalog No. T22893 CAS 191034-25-0

Synonyms: L-168,049

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.

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L-168049, CAS 191034-25-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 189.00
25 mg	In stock	$ 397.00
50 mg	In stock	$ 589.00
100 mg	In stock	$ 843.00
500 mg	In stock	$ 1,730.00
1 mL * 10 mM (in DMSO)	In stock	$ 125.00

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Purity: 100%

Biological Description

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Description	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.
Targets&IC50	Glucagon receptor (canine):60 nM (IC50), Glucagon receptor (murine):63 nM (IC50), Glucagon receptor (human):3.7 nM (IC50)
In vitro	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 vivo	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].

Synonyms	L-168,049
Molecular Weight	467.79
Formula	C24H20BrClN2O
CAS No.	191034-25-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3.4mM

DMSO: insoluble

References and Literature

1. M A Cascieri, et al. Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J Biol Chem. 1999 Mar 26;274(13):8694-7. 2. Elodie Mutel, et al. Control of blood glucose in the absence of hepatic glucose production during prolonged fasting in mice: induction of renal and intestinal gluconeogenesis by glucagon. Diabetes. 2011 Dec;60(12):3121-31. 3. S E de Laszlo, et al. Potent, orally absorbed glucagon receptor antagonists. Bioorg Med Chem Lett. 1999 Mar 8;9(5):641-6.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

L-168049 191034-25-0 GPCR/G Protein Glucagon Receptor L168049 L-168,049 L 168049 inhibitor inhibit

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