1391737-01-1
基本信息
化合物VU0463271
Inhibitor,KcsA,VU0463271,Potassium Channel,VU 0463271,VU-0463271,inhibit
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]-
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)
VU0463271 (Synonyms: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)
物理化学性质
| 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 |
安全数据
| WGK Germany | WGK 3 |
| 存储类别 | 11 - Combustible Solids |
VU 0463271价格(试剂级)
| 报价日期 | 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 |
| 2026/09/15 | HY-110110 | VU 0463271 VU0463271 | 1391737-01-1 | 10 mg | 718元 |
常见问题列表
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.