| 货号 | 16967-25mg |
| 描述 | Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM.1 It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 µM).2 Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been used to study long QT syndrome type 2.3,4 Furthermore, because it can target oncogenic ERG1 and ERG potassium channels, astemizole has been explored as a potential antineoplastic agent for decreasing proliferation of various cancer cells.5 |
| 别名 | NSC 329963; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ahn, H.S. and Barnett, A. Selective displacement of [3H]mepyramine from peripheral vs. central nervous system receptors by loratadine, a non-sedating antihistamine. European Journal of Pharmacology 127(1-2), 153-155 (1986). 2.Kubo, N.,Shirakawa, S.,Kuno, T., et al. Antimuscarinic effects of antihistamines: Quantitative evaluation by receptor-binding assay. Japanese Journal of Pharmacology 43(3), 277-282 (1987). 3.Du, L.P.,Tsai, K.C.,Li, M.Y., et al. The pharmacophore hypotheses of IKr potassium channel blockers: Novel class III antiarrhythmic agents. Bioorg. Med. Chem. Lett. 14(18), 4771-4777 (2004). 4.Ficker, E.,Obejero-Paz, C.A.,Zhao, S., et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. The Journal of Biological Chemisty 277(7), 4989-4998 (2002). 5.García-Quiroz, J.,García-Becerra, R.,Santos-Martínez, N., et al. In vivo dual targeting of the oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results in enhanced antineoplastic effects in breast tumors. BMC Cancer 14, 2-10 (2014). | |
| 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 | 458.6 |
| 分子式 | C28H31FN4O |
| CAS号 | 68844-77-9 |
| 稳定性 | ≥ 2 years |
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