L-168,049

Product Description

L-168,049 is a very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC₅₀ = 3.7 nM), and moderate affinity to murine and canine GRs (IC₅₀ values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC₅₀ > 1 μM). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC₅₀ = 41 nM), and in murine liver membranes. Orally active in vivo.

Solubility

Preparing Stock Solutions for L-168,049

The following data is based on the product molecular weight 467.79

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.14 mL	10.69 mL	21.38 mL
5 mM	0.43 mL	2.14 mL	4.28 mL
10 mM	0.21 mL	1.07 mL	2.14 mL
50 mM	0.04 mL	0.21 mL	0.43 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• de Laszlo Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 1999 PMID: 10201821
• Dallas-Yang Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem.
• Cascieri Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 1999 PMID: 10085108