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VU0463271  99.1781%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(25mg/ml 超声)
产品描述：基本信息 产品编号： V10156 产品名称： VU0463271 CAS: 1391737-01-1   储存条件 粉末 -20℃ 四年     分子式： C19H18N4Os2 溶于液体 -80℃ 6个月 分子量： 382.50 -20℃ 1个月 化学名：  N-Cyclopropyl-N-(4-methyl-thiazol-2-yl)-2-(6-phenyl-pyridazin-3-ylsulfanyl)-acetamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6144mL 13.0719mL 26.1438mL 5mM 0.5229mL 2.6144mL 5.2288mL 10mM 0.2614mL 1.3072mL 2.6144mL   生物活性 产品描述 一种选择性的神经特异性氯钾协同转运蛋白2(KCC2)的有效抑制剂。 靶点 IC50:61nM (KCC2).   体外研究 VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2),with an IC50 of 61nM 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 1μM 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 (10-100nM) results in approximately 20% reduction of CNS firing frequency within asmall percentage of preparations. 体内研究 VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57mL/min/kg) following intravenous administration (1mg/kg);the low volume of distribution at steady state (Vss 0.4L/kg),coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo.
保存条件：-20℃

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