Molecular structure of L-168,049, CAS Number: 191034-25-0
L-168,049 (CAS 191034-25-0)
Alternate Names:
Glucagon Receptor Antagonist II; 2-(4-Pyridyl)-5-(4-Chlorophenyl)-3-(5-Bromo-2-Propyloxyphenyl)Pyrrole;
Application:
L-168,049 is a non-peptidyl human glucagon receptor antagonist
CAS Number:
191034-25-0
Purity:
≥99%
Molecular Weight:
467.79
Molecular Formula:
C24H20BrClN2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
L-168,049 is a potent, selective and non-competitive antagonist of the human glucagon receptor (hGR). It 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).
L-168,049 (CAS 191034-25-0) References
- Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. | Cascieri, MA., et al. 1999. J Biol Chem. 274: 8694-7. PMID: 10085108
- Potent, orally absorbed glucagon receptor antagonists. | de Laszlo, SE., et al. 1999. Bioorg Med Chem Lett. 9: 641-6. PMID: 10201821
- Generation of mice expressing the human glucagon receptor with a direct replacement vector. | Shiao, LL., et al. 1999. Transgenic Res. 8: 295-302. PMID: 10621976
- Detection of glucagon-dependent GTPgammaS binding in high-throughput format. | Dallas-Yang, Q., et al. 2002. Anal Biochem. 301: 156-9. PMID: 11811981
- Glucagon signaling modulates sweet taste responsiveness. | Elson, AE., et al. 2010. FASEB J. 24: 3960-9. PMID: 20547661
- Structure-based discovery of allosteric modulators of two related class B G-protein-coupled receptors. | de Graaf, C., et al. 2011. ChemMedChem. 6: 2159-69. PMID: 21994134
- Rescue of a pathogenic mutant human glucagon receptor by pharmacological chaperones. | Yu, R., et al. 2012. J Mol Endocrinol. 49: 69-78. PMID: 22693263
- Involvement of Glucagon in Preventive Effect of Menthol Against High Fat Diet Induced Obesity in Mice. | Khare, P., et al. 2018. Front Pharmacol. 9: 1244. PMID: 30505271
- GLP-1 metabolite GLP-1(9-36) is a systemic inhibitor of mouse and human pancreatic islet glucagon secretion. | Gandasi, NR., et al. 2024. Diabetologia. 67: 528-546. PMID: 38127123
- Sex-dependent intra-islet structural rearrangements affecting alpha-to-beta cell interactions lead to adaptive enhancements of Ca2+ dynamics in prediabetic beta cells. | Visa, M. and Berggren, PO. 2024. Diabetologia.. PMID: 38814444
Inhibitor of:
Glucagon Receptor, and secretin receptor.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
L-168,049, 10 mg | sc-204034 | 10 mg | $170.00 | |||
| US: Only available in the US | ||||||
L-168,049, 50 mg | sc-204034A | 50 mg | $700.00 | |||
| US: Only available in the US | ||||||