| Name | L-168,049 |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 1856 |
| Prices | $159.00, $665.00 |
| Sizes | 10 mg, 50 mg |
| Function Type | Antagonist |
| Cas Number | 191034-25-0 |
| Chemical Name | 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine |
| Formula | C24H20BrClN2O |
| Molecular Weight | 467.79 |
| Purity | >99 % |
| Description | Very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC 50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC 50 values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC 50 > 1 μ M). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC 50 = 41 nM), and in murine liver membranes. Orally active in vivo . |
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Cascieri MA, Koch GE, Ber E, Sadowski SJ, Louizides D, de Laszlo SE, Hacker C, Hagmann WK, MacCoss M, Chicchi GG, Vicario PP. J Biol Chem. 1999 Mar 26;274(13):8694-7.
de Laszlo SE, Hacker C, Li B, Kim D, MacCoss M, Mantlo N, Pivnichny JV, Colwell L, Koch GE, Cascieri MA, Hagmann WK. Bioorg Med Chem Lett. 1999 Mar 8;9(5):641-6.