| 货号 | 15223-50mg |
| 描述 | The G protein-coupled receptors GPR109A and GPR109B are recognized to be receptors for hydroxy-carboxylic acid (HCA) metabolites, are abundant in adipocytes, and are relevant to atherosclerosis and dyslipidemia.1,2 IPBT-5CA is a selective agonist of GPR109B (HCA3; EC50 = 400 nM).3 It displays no activity at GPR109A (HCA2).3 IBC-293 inhibits forskolin-stimulated cAMP release in Chinese hamster ovary cells stably expressing GPR109B (EC50 = 54 nM) but not in cells expressing GPR109A.4 This is accompanied by a rapid and transient increase in intracellular calcium and activation of ERK1/2 through a pertussis toxin-sensitive Gi signaling pathway.4 |
| 别名 | IBC-293; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ahmed, K.,Tunaru, S. and Offermanns, S. GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors. Trends in Pharamacological Sciences 30(11), 557-562 (2009). 2.Offermanns, S.,Colletti, S.L.,Lovenberg, T.W., et al. International union of basic and clinical pharmacology. LXXXII: Nomenclature and classification of hydroxy-carboxylic acid receptors (GPR81, GPR109A, and GPR109B). Pharmacological Reviews 63(2), 269-290 (2011). 3.Semple, G.,Skinner, P.J.,Cherrier, M.C., et al. 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b. Journal of Medicinal Chemistry 49(4), 1227-1230 (2006). 4.Zhou, Q.,Li, G.,Deng, X.Y., et al. Activated human hydroxy-carboxylic acid receptor-3 signals to MAP kinase cascades via the PLC-dependent PKC and MMP-mediated EGFR pathways. British Journal of Pharmacology 166(6), 1756-1773 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 205.2 |
| 分子式 | C10H11N3O2 |
| CAS号 | 306935-41-1 |
| 稳定性 | ≥ 2 years |
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