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SKA-31
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SKA-31
CAS No. : 40172-65-4
MCE 站:SKA-31
产品活性: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。
研究领域:Membrane Transporter/Ion Channel
作用靶点:Potassium Channel
In Vitro: 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.
In Vivo: 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 (-/-).
相关产品:Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Anti-Cardiovascular Disease Compound Library | Neuroprotective Compound Library | Nigericin sodium salt | BAPTA-AM | Rosuvastatin Calcium | SKF-96365 hydrochloride | Glibenclamide | SCH-23390 hydrochloride | Tetrandrine | Amiodarone hydrochloride | TRAM-34 | Ifenprodil tartrate | Minoxidil | Diazoxide | 20(S)-Ginsenoside Rg3 | Senicapoc | Tannic acid | DCPIB | Astemizole | Ketanserin | Quinine | E-4031 | Terfenadine | Hydrochlorothiazide | GW9508 | Daurisoline | Nicorandil | Dofetilide | Pinacidil monohydrate | ML277 | Tolbutamide | Almitrine mesylate
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