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SKA-31

SKA-31

产品编号 T5180   CAS 40172-65-4
别名: SKA31, Naphtho[1,2-d]thiazol-2-ylamine, SKA 31

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。

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SKA-31 Chemical Structure
SKA-31, CAS 40172-65-4
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
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产品目录号及名称: SKA-31 (T5180)
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL (150 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Sankaranarayanan A, Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure. Mol Pharmacol. 2009 Feb;75(2):281-95. 2. Hasenau AL, et al. Improvement of endothelium-dependent vasodilations by SKA-31 and SKA-20, activators of small- and intermediate-conductance Ca2+ -activated K+ -channels. Acta Physiol (Oxf). 2011 Sep;203(1):117-26. 3. Mishra RC, et al. Inhibition of Myogenic Tone in Rat Cremaster and Cerebral Arteries by SKA-31, an Activator of Endothelial KCa2.3 and KCa3.1 Channels. J Cardiovasc Pharmacol. 2015 Jul;66(1):118-27.
Talatisamine Dimethindene Cisapride Daurisoline Dofetilide Pimozide Alismol TKIM

相关化合物库

该产品包含在如下化合物库中:
离子通道库 抗癌化合物库 已知活性化合物库 NO PAINS 化合物库 钾通道分子库 经典已知活性库

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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。

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Keywords

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

 

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