VU0463271|cas:1391737-01-1|西域试剂

VU0463271,98.06%

产品编号：Bellancom-110110| CAS NO：1391737-01-1| 分子式：C₁₉H₁₈N₄OS₂| 分子量：382.50

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货号	价格	库存与货期
Bellancom-110110	￥900.00	杭州北京（现货）
Bellancom-110110	￥1500.00	杭州北京（现货）
Bellancom-110110	￥3300.00	杭州北京（现货）
Bellancom-110110	￥5300.00	杭州北京（现货）
Bellancom-110110	￥8500.00	杭州北京（现货）

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VU0463271

产品介绍

VU0463271 是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，其 IC₅₀ 值为 61 nM。

生物活性

VU0463271 is a selective 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 : 25 mg/mL (65.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6144 mL	13.0719 mL	26.1438 mL
5 mM	0.5229 mL	2.6144 mL	5.2288 mL
10 mM	0.2614 mL	1.3072 mL	2.6144 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。