SKA-31

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Chemical Structure| 40172-65-4 同义名 : 2-Aminonaphthiazole
CAS号 : 40172-65-4
货号 : A226793
分子式 : C11H8N2S
纯度 : 98%
分子量 : 200.26
MDL号 : MFCD00051329
存储条件:

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
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

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