VU0463271 quarterhydrate|西域试剂

VU0463271 quarterhydrate,98.0%

产品编号：Bellancom-110110A| 分子式：C₁₉H₁₈N₄OS₂.1/4H₂O| 分子量：387.00

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-110110A		￥2500.00	杭州北京（现货）

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VU0463271 quarterhydrate

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 potent KCC2 antagonist, with an IC₅₀ of 61 nM.

体外研究

VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC₅₀ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式