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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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree 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|
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
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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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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.