货号 | 5380/50 |
别名 | N-(3,4-Difluorophenyl)-N'-(3-methyl- |
供应商 | Tocris |
生物活性 | Selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). Exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters. Prevents PTZ-induced epileptic seizures in mice. Brain penetrant. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >99 % |
计算分子量 | 328.32 |
分子式 | C17H14F2N4 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
参考文献 | Kaufmannet al (2013) ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem.Neurosci. 4 1278. PMID: 23730969. Wenet al (2013) Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg.Med.Chem.Lett. 23 4562. PMID: 23838260. |