VU0463271 quarterhydrate

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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。

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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	2.5840 mL	12.9199 mL	25.8398 mL
5 mM	0.5168 mL	2.5840 mL	5.1680 mL
10 mM	0.2584 mL	1.2920 mL	2.5840 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。