SKA-31  ≥98%

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包装规格:100mg 250mg 1g in glass bottle
溶解性:溶于DMSO(150mg/ml 超声)
产品描述:基本信息 产品编号: S10975  产品名称: SKA-31 CAS: 40172-65-4   储存条件 粉末 2-8℃ 四年 分子式: C11H8N2S 溶于液体 -80℃ 6个月 分子量: 200.26 -20℃ 1个月 化学名:  SKA 31;SKA31;Naphtho[1,2-d]thiazol-2-ylamine;2-Amino-beta-naphthothiazole;2-Aminonaphthiazole Solubility (25°C):   体外:   DMSO   Ethanol 'mg/mL Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.9935mL 24.9675mL 49.9351mL 5mM 0.9987mL 4.9935mL 9.9870mL 10mM 0.4994mL 2.4968mL 4.9935mL   生物活性 产品描述 一种钾离子通道(potassiumchannel)激活剂,能增强内皮源性超极化因子反应,降低血压。 靶点 EC50:2.9μM (KCa2.1),1.9μM (KCa2.2),2.9μM (KCa2.3),260nM (KCa3.1)   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 5.3μM,46.9μM in HCT-116 cells and HCT-8 cells,respectively.SKA-31 (5.3μM;0-96 hours) reduces HCT-116 cells proliferation when added at time zero at 5.3μM.SKA-31 triggers apoptosis in HCT-116 cells at 5μM,and the effect is smaller in HCT-8 cells at 45μM.SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5μM and 45μM,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. Cell Viability Assay Cell Line: HCT-116 cells,HCT-8 cells Incubation Time: 24 hours Result: Reduced cell viability with IC50s of 5.3μM, 46.9μM in HCT-116 and HCT-8,respectively. Cell Proliferation Assay Cell Line: HCT-116 cells Concentration: 5.3μM Incubation Time: 0-96 hours Result: Reduced HCT-116 cells proliferation when added at time zero at IC50S value. Apoptosis Analysis Cell Line: HCT-116 cells,HCT-8 cells Concentration: 5μM (HCT-116 cells),45μM (HCT-8 cells) Incubation Time: 24 hours Result: Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells. Cell Cycle Analysis Cell Line: HCT-116 cells,HCT-8 cells Concentration: 5μM (HCT-116),45μM (HCT-8) Incubation Time: 24 hours Result: Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines. Western Blot Analysis Cell Line: HCT-116 cells Incubation Time: 24 hours Result: Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells. 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 225nM and 1.6μM 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 (1-30mg/kg;i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-). Animal Model: 16-25 weeks mice Dosage: 1mg/kg,10mg/kg,and 30mg/kg Administration: Intraperitoneal injection Result: Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-)mice (-/-).
保存条件:2-8℃