Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) 是一种钾离子通道激活剂,作用于 KCa3.1,KCa2.2,KCa2.1和 KCa2.3的 EC50分别为 260 nM,1.9 μM,2.9 μM,2.9 μM. SKA31增强内皮源性超极化因子反应,降低血压。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 496 | 现货 | ||
10 mg | ¥ 825 | 现货 | ||
25 mg | ¥ 1,530 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 555 | 现货 |
产品描述 | SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) is an activator of KCa3.1 and KCa2 channels (EC50s: 260, 2900, 2900 nM for KCa3.1, KCa2.1 and KCa2.2 respectively). |
靶点活性 | KCa3.1:260 nM, KCa2.1:2900 nM, KCa2.2:2900 nM |
体外活性 | SKA-31 activates KCa2.1 with EC(50) values of 2.9 microM, KCa2.2 with an EC(50) value of 1.9 microM, KCa2.3 with EC(50) values of 2.9 microM, and KCa3.1 with EC(50) values of 260 nM. SKA-31 activated native KCa2.3 and KCa3.1 channels in murine endothelial cells [1]. SKA-31 (1 μM) activated KCa3.1 and KCa2.3 channels and induced membrane hyperpolarization in CAEC of wt (ΔMP -45 mV). SKA-31 (200 nM, 500 nM) significantly enhanced EDHF vasodilations in wt [2]. |
体内活性 | 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 [2]. SKA-31 (10 μM) inhibited myogenic tone by 80% in cremaster and ~65% in middle cerebral arteries, with IC50 values of ~2 μM in both vessels [3]. |
细胞实验 | Jurkat E61 and MEL cells were seeded at 10^5 cells/ml in 12-well plates. SKA-31 was added at concentrations of 10 and 100 μM in a final DMSO concentration of 0.1%, which was found not to affect cell viability. After 48 h, the cells in each well were well mixed and resuspended, and the number of trypan blue-positive cells in three aliquots from each well was determined under a light microscope. The test was repeated twice [1]. |
动物实验 | For intravenous injection, SKA-31 was dissolved at 10 mg/ml in a mixture of 10% Cremophor EL and 90% saline and injected at 10 mg/kg. For intraperitoneal application, SKA-31 was dissolved at 10 mg/ml in Miglyol 812 neutral oil (caprylic/capric triglyceride). After tail vein injection of the aqueous solution or intraperitoneal administration of the oily solution, approximately 200 μl of blood was collected from the tail into EDTA blood sample collection tubes at various time points. For very early time points (3, 5, and 10 min) after intravenous administration, blood samples were obtained by cardiac puncture under deep isoflurane anesthesia. Plasma was separated by centrifugation and stored at -80°C pending analysis. After determining that SKA-31 plasma concentrations peaked 2 h after application (10 mg/kg i.p.), we took blood samples under deep isoflurane anesthesia by cardiac puncture from a group of three rats before sacrificing the animals to remove brain, heart, liver, spleen, and fat. Tissue samples were homogenized in 1 ml of H2O with a homogenizer, and the protein was precipitated with 1 ml of acetonitrile. The samples were then centrifuged at 3000 rpm, and supernatants were concentrated to 1 ml. Plasma and homogenized tissue samples were purified using C18 solid-phase extraction cartridges. Elution fractions corresponding to SKA-31 were evaporated to dryness under nitrogen and dissolved in acetonitrile [1]. |
别名 | SKA31, Naphtho[1,2-d]thiazol-2-ylamine, SKA 31 |
分子量 | 200.26 |
分子式 | C11H8N2S |
CAS No. | 40172-65-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (150 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.9935 mL | 24.9675 mL | 49.9351 mL | 124.8377 mL |
5 mM | 0.9987 mL | 4.9935 mL | 9.987 mL | 24.9675 mL | |
10 mM | 0.4994 mL | 2.4968 mL | 4.9935 mL | 12.4838 mL | |
20 mM | 0.2497 mL | 1.2484 mL | 2.4968 mL | 6.2419 mL | |
50 mM | 0.0999 mL | 0.4994 mL | 0.9987 mL | 2.4968 mL | |
100 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2484 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SKA-31 40172-65-4 Membrane transporter/Ion channel Potassium Channel inhibit SKA31 Naphtho[1,2-d]thiazol-2-ylamine SKA 31 KcsA Inhibitor inhibitor