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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)
Citations (1)
Literature (1)

Biological Activity for L-168,049

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.

Compound Libraries for L-168,049

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Technical Data for L-168,049

M. Wt 467.79
Formula C24H20BrClN2O
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 191034-25-0
PubChem ID 5311276
Smiles CCCOC1=C(C=C(Br)C=C1)C1=C(NC(=C1)C1=CC=C(Cl)C=C1)C1=CC=NC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for L-168,049

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.78 100
ethanol 46.78 100

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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References for L-168,049

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

Cascieri et al (1999) Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 274 8694 PMID: 10085108

de Laszlo et al (1999) Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 9 641 PMID: 10201821

Dallas-Yang et al (2001) Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem. 301 156

If you know of a relevant reference for L-168,049, please let us know.

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Keywords: L-168,049, L-168,049 supplier, Potent, orally, active, human, glucagon, receptor, antagonists, Receptors, L168049, Glucagon, Receptor, 2311, Tocris Bioscience

1 Citation for L-168,049

Citations are publications that use Tocris products. Selected citations for L-168,049 include:

Rodriguez-Diaz et al (2018) Paracrine Interactions within the Pancreatic Islet Determine the Glycemic Set Point. Cell Metab 27 549 PMID: 29514065

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.