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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
40172-65-4
- 规格:
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥770.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥600.0 |
| 规格: | 10 mg | 产品价格: | ¥1000.0 |
| 规格: | 50 mg | 产品价格: | ¥3000.0 |
| 规格: | 100 mg | 产品价格: | ¥4800.0 |
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SKA-31
CAS No. : 40172-65-4
MCE 国际站: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.
?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 (-/-).
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文献和实验27 4.24 3.65 3.31 3.08 2.92 2.80 2.71 2.63 2.57 2.47 2.36 2.25 2.13 2.00 1.85 27 28 4.22 3.63 3.29 3.06 2.90 2.78 2.69 2.61 2.55 2.45 2.34 2.23 2.11 1.98 1.83 28 29 4.20 3.61 3.27 3.04 2.88 2.76 2.67 2.59 2.53 2.43 2.32 2.21 2.09 1.96 1.81 29
. We also use these data to construct approximate genome scaffolds de novo. Applying our approach to incomplete regions of the human genome, we predict the positions of 65 previously unplaced contigs, in agreement with alternative methods in 26/31 cases
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