NS8593 hydrochloride|cas:875755-24-1|西域试剂

NS8593 hydrochloride,99.81%

产品编号：Bellancom-110105| CAS NO：875755-24-1| 分子式：C₁₇H₁₈ClN₃| 分子量：299.80

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货号	价格	库存与货期
Bellancom-110105	￥1000.00	杭州北京（现货）
Bellancom-110105	￥1950.00	杭州北京（现货）
Bellancom-110105	￥4500.00	杭州北京（现货）

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NS8593 hydrochloride

产品介绍

NS8593 hydrochloride 是一种有效的选择性的 SK channels (小电导钙激活钾通道)抑制剂。NS8593 hydrochloride 可逆地抑制 SK3 介导的电流，K_d 值为 77 nM。NS8593 hydrochloride 抑制所有 SK1-3 亚型的 Ca²⁺ 依赖性 (在 0.5 μM Ca²⁺ 时，K_d 分别为 0.42、0.60 和 0.73 μM)，并且不影响中间电导和大电导的钙激活钾通道 (分别为 hIK 和 hBK 通道)。

生物活性

NS8593 hydrochloride is a potent and selective small conductance Ca²⁺-activated K⁺ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a K_d value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca²⁺-dependently (K_ds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca²⁺), and does not affect the Ca²⁺-activated K⁺ channels of intermediate and large conductance (hIK and hBK channels, respectively).

体外研究

When tested in excised patches, it is found that the inhibition by NS8593 (compound 14) decreased as the intracellular [Ca²⁺] is increased and that NS8593 is equipotent when applied from either the intracellular or the extracellular side of the cell membrane. A HEK293 cell transiently transfected with hSK3 channels is inhibited by 80% upon application of 100 nM apamin and by 75% after application of 300 nM NS8593. In contrast, NS8593 inhibits the mutated channel by 45% at 300 nM. NS8593 thus remains active on the apamin-insensitive SK3 channel, although the K_d value of 0.43 µM is 4-fold higher than found for a wild-type hSK3 channel (K_d of 0.10 µM). As the potency of NS8593 is dependent on the degree of SK3 channel activation, the decreased potency could thus reflect an increased apparent Ca²⁺-sensitivity of the mutated channels. Similar to the whole-cell experiments, the potency of NS8593 is reduced 3-fold from 0.67 µM to 2.2 µM when tested at a Ca²⁺ concentration of 500 nM.

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

体内研究

NS8593 (compound 14) (3 and 10 mg/kg intravenously) is able to affect firing rate and firing pattern of dopaminergic neurons in vivo in C57Bl/6 mice.

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

体内研究

NS8593 (compound 14) (3 and 10 mg/kg intravenously) is able to affect firing rate and firing pattern of dopaminergic neurons in vivo in C57Bl/6 mice.

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 : 83.33 mg/mL (277.95 mM; Need ultrasonic)

H₂O : 1 mg/mL (3.34 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3356 mL	16.6778 mL	33.3556 mL
5 mM	0.6671 mL	3.3356 mL	6.6711 mL
10 mM	0.3336 mL	1.6678 mL	3.3356 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 (sealed storage, away from moisture)。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.94 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.94 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.94 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。