SKA-31,40172-65-4

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抑制剂描述：

产品名称：SKA-31

产品别名：见爱必信官网

英文别名：SKA-31

靶点：Potassium Channel

CAS：40172-65-4

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

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.

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

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 IC50s 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.

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.

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