| 货号 | 2311/50 |
| 别名 | 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4 |
| 供应商 | Tocris |
| 生物活性 | 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. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >99 % |
| 计算分子量 | 467.79 |
| 分子式 | C24H20BrClN2O |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| CAS号 | 191034-25-0 |
| 参考文献 | Dallas-Yanget al (2001) Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem. 301156. 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. |