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SKA-31 {[allProObj[0].p_purity_real_show]}

货号:A226793 同义名: 2-Aminonaphthiazole

SKA 31 is an activator of KCa3.1 and KCa2 channels with EC50 of 260, 2900, 2900 nM for KCa3.1, KCa2.1 and KCa2.2 respectively.

SKA-31 化学结构 CAS号:40172-65-4
SKA-31 化学结构
CAS号:40172-65-4
SKA-31 3D分子结构
CAS号:40172-65-4
SKA-31 化学结构 CAS号:40172-65-4
SKA-31 3D分子结构 CAS号:40172-65-4
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SKA-31 纯度/质量文件 产品仅供科研

货号:A226793 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

97%
Dronedarone Hydrochloride 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

98%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

98%
Glibenclamide 98%
Amiodarone HCl 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

98%
Repaglinide 98%
Dofetilide 98%
Nateglinide 99%
Quinine hydrochloride dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

SKA-31 生物活性

描述 SKA-31 is a potent potassium channel activator with EC50s 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. SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other ion channels. 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. Administration of 10 and 30 mg/kg SKA-31 lowered mean arterial blood pressure by 4 and 6 mm Hg in normotensive mice and by 12 mm Hg in angiotensin-II-induced hypertension. SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation[1]. SKA-31 reduces cell viability with IC50s of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively. 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[2].

SKA-31 参考文献

[1]Sankaranarayanan A, Raman G, Busch C, et al. Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure. Mol Pharmacol. 2009;75(2):281-295

[2]Pillozzi S, D'Amico M, Bartoli G, et al. The combined activation of KCa3.1 and inhibition of Kv11.1/hERG1 currents contribute to overcome Cisplatin resistance in colorectal cancer cells. Br J Cancer. 2018;118(2):200-212

SKA-31 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.99mL

1.00mL

0.50mL

24.97mL

4.99mL

2.50mL

49.94mL

9.99mL

4.99mL

SKA-31 技术信息

CAS号40172-65-4
分子式C11H8N2S
分子量 200.26
别名 2-Aminonaphthiazole
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 120 mg/mL(599.22 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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