| 货号 | 19353-50mg |
| 描述 | VU0255035 is a competitive, orthosteric antagonist of the muscarinic M1 receptor (IC50 = 130 nM).1,2 It displays at least 75-fold selectivity for M1 over other muscarinic receptors, as well as a panel of receptors, ion channels, and transporters.1,2 VU0255035 is effective in cells and in vivo and brain penetrating, blocking pilocarpine-induced seizures without disrupting contextual fear conditioning in mice.1,2 VU0255035 is used to examine the role of the M1 receptor in diverse situations.3,4,5 |
| 别名 | ML-012; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sheffler, D.J.,Williams, R.,Bridges, T.M., et al. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Molecular Pharmacology 76(2), 356-368 (2009). 2.Weaver, C.D.,Sheffler, D.J.,Lewis, L.M., et al. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe. Current Topics in Medicinal Chemistry 9(13), 1217-1226 (2009). 3.Shirey, J.K.,Brady, A.E.,Jones, P.J., et al. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. Journal of Neuroscience 29(45), 14271-14286 (2009). 4.Xiang, Z.,Thompson, A.D.,Jones, C.K., et al. Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson’s disease. Journal of Pharmacology and Experimental Therapeutics 340(3), 595-603 (2012). 5.Harada, K.,Matsuoka, H.,Miyata, H., et al. Identification of muscarinic receptor subtypes involved in catecholamine secretion in adrenal medullary chromaffin cells by genetic deletion. British Journal of Pharmacology 172(5), 1348-1359 (2015). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 432.5 |
| 分子式 | C18H20N6O3S2 |
| CAS号 | 1135243-19-4 |
| 稳定性 | ≥ 1 year |
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