SKA-31 - CAS:40172-65-4

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SKA-31

目录号 : KM6376 CAS No. : 40172-65-4 纯度 : 98%

Data Sheet 产品使用指南

SKA-31 是钾离子通道 (potassium channel) 激活剂，作用于 KCa3.1，KCa2.2，KCa2.1 和 KCa2.3 的 EC₅₀ 值分别为 260 nM，1.9 μM，2.9 μM，2.9 μM，能增强内皮源性超极化因子反应，降低血压。

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生物活性

SKA-31 is a potent potassium channel activator with EC_50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.

体外研究

SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other Ion channels.
SKA-31 reduces cell viability with IC_50s of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively.
SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation when added at time zero at 5.3 μM.
SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM.
SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively.
SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by CDDP.
SKA-31 has a synergic effect with CDDP also on the inhibition of HCT-116 cell proliferation.

Cell Viability Assay

Cell Line:	HCT-116 cells, HCT-8 cells
Concentration:
Incubation Time:	24 hours
Result:	Reduced cell viability with IC_50s of 5.3 μM , 46.9 μM in HCT-116 and HCT-8, respectively.

Cell Proliferation Assay

Cell Line:	HCT-116 cells
Concentration:	5.3 μM
Incubation Time:	0-96 hours
Result:	Reduced HCT-116 cells proliferation when added at time zero at IC_50S value.

Apoptosis Analysis

Cell Line:	HCT-116 cells, HCT-8 cells
Concentration:	5 μM (HCT-116 cells), 45 μM (HCT-8 cells)
Incubation Time:	24 hours
Result:	Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells.

Cell Cycle Analysis

Cell Line:	HCT-116 cells, HCT-8 cells
Concentration:	5 μM (HCT-116), 45 μM (HCT-8)
Incubation Time:	24 hours
Result:	Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines.

Western Blot Analysis

Cell Line:	HCT-116 cells
Concentration:
Incubation Time:	24 hours
Result:	Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells.

体内研究

SKA-31 is not acutely toxic and has good pharmacokinetic properties.
SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC₅₀ values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively.
SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation.
SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).

Animal Model:	16-25 weeks mice
Dosage:	1 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:	Intraperitoneal injection
Result:	Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).

分子式

C₁₁H₈N₂S

分子量

200.26

CAS号

40172-65-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 150 mg/mL (749.03 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.9935 mL	24.9675 mL	49.9351 mL
5 mM	0.9987 mL	4.9935 mL	9.9870 mL
10 mM	0.4994 mL	2.4968 mL	4.9935 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (12.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (12.48 mM，饱和度未知) 的澄清溶液。
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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (12.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (12.48 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。