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VU0463271 quarterhydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VU0463271 quarterhydrate图片
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
VU0463271 quarterhydrate 是神经特异性氯钾协同转运蛋白 2(KCC2)的有效抑制剂,其IC50值为 61 nM。
生物活性

VU0463271 quarterhydrate is a potentKCC2antagonist, with anIC50of 61 nM[1].

IC50& Target

IC50: 61 nM (KCC2)[1].

体外研究
(In Vitro)

VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50of 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[1].
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[2].
VU0463271 (10-100 nM) results in approximately 20% reduction of CNS firing frequency within a small percentage of preparations[2].

体内研究
(In Vivo)

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[1].

分子量

387.00

性状

Solid

Formula

C19H18N4OS2.1/4H2O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 19 mg/mL(49.10 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5840 mL12.9199 mL25.8398 mL
5 mM0.5168 mL2.5840 mL5.1680 mL
10 mM0.2584 mL1.2920 mL2.5840 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。