Description: Potent, orally active human glucagon receptor antagonist
Chemical Name: 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
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.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
46.78
100
ethanol
46.78
100
Preparing Stock Solutions
The following data is based on the product molecular weight 467.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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
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Product Datasheets
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Cascieriet al (1999) Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 274 8694 PMID: 10085108
de Laszloet al (1999) Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 9 641 PMID: 10201821
Dallas-Yanget al (2001) Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem. 301 156 PMID: