VU 0463271
| 中文名称 | VU 0463271 |
|---|---|
| 中文同义词 | 化合物 T17243;化合物VU0463271;N-环丙基-N-(4-甲基-2-噻唑基)-2-[(6-苯基-3-哒嗪基)硫基]乙酰胺;化合物VU0463271,10 MM DMSO 溶液;N-环丙基-N-(4-甲基噻唑-2-基)-2-((6-苯基哒嗪-3-基)硫代)乙酰胺 |
| 英文名称 | VU 0463271 |
| 英文同义词 | VU 0463271;VU0463271 (Synonyms: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide);N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide;VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide);Acetamide, N-cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-;Inhibitor,KcsA,VU0463271,Potassium Channel,VU 0463271,VU-0463271,inhibit;VU0463271, 10 mM in DMSO;N-Cyclopropyl-N-(4-methylthiazol-2-yl)-2-((6-phenylpyridazin-3-yl)thio)acetamide |
| CAS号 | 1391737-01-1 |
| 分子式 | C19H18N4OS2 |
| 分子量 | 382.5 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1391737-01-1.mol |
| 结构式 |  |
VU 0463271 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 颜色 | 灰白色至蓝灰色 |
| InChI | 1S/C19H18N4OS2/c1-13-11-26-19(20-13)23(15-7-8-15)18(24)12-25-17-10-9-16(21-22-17)14-5-3-2-4-6-14/h2-6,9-11,15H,7-8,12H2,1H3 |
| InChIKey | DPONSKCACOZTGN-UHFFFAOYSA-N |
| SMILES | [s]1c(nc(c1)C)N(C4CC4)C(=O)CSc2nnc(cc2)c3ccccc3 |
IC50: 61 nM (KCC2).
VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC
50
of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters. It is also found rapidly cleared in vitro.
VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively.
VU0463271 (10-100 nM) results in approximately 20% reduction of CNS firing frequency within a
small percentage of preparations.
VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg) following intravenous administration (1 mg/kg); the low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo.
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-110110 | VU 0463271 VU0463271 | 1391737-01-1 | 5mg | 418元 |
| 2026/09/15 | HY-110110 | VU0463271 | 1391737-01-1 | 10 mM * 1 mLin DMSO | 459元 |