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  • 化合物 SKA-31|T5180|TargetMol

化合物 SKA-31|T5180|TargetMol

SKA-31
40172-65-4
131 1mg 起订
298 5mg 起订
495 10mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 SKA-31
英文名称:
SKA-31
CAS号:
40172-65-4
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.38%
产品类别:
抑制剂
货号:
T5180

Product Introduction

Bioactivity

名称SKA-31
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).
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].
体外活性SKA-31能夠激活KCa2.1,其EC(50)值為2.9 microM;KCa2.2的EC(50)值為1.9 microM;KCa2.3的EC(50)值為2.9 microM;以及KCa3.1的EC(50)值為260 nM。SKA-31在小鼠内皮细胞中激活了天然的KCa2.3和KCa3.1通道[1]。SKA-31 (1 μM)能夠激活KCa3.1以及KCa2.3通道,并在野生型CAEC中引起膜超极化(ΔMP -45 mV)。SKA-31(200 nM、500 nM)顯著增强了野生型中EDHF引起的血管舒張[2]。
体内活性给予10和30 mg/kg的SKA-31可以分别将正常血压小鼠的平均动脉血压降低4和6 mm Hg,并且在由血管紧张素II引起的高血压中可以降低12 mm Hg [2]。SKA-31 (10 μM) 在阴囊的微血管及中脑动脉中抑制肌肉舒张力分别高达80%和约65%,两种血管的IC50值均约为2 μM [3]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 30 mg/mL (150 mM)
关键字inhibit | Potassium Channel | KcsA | Inhibitor | SKA-31
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SKA31|||Naphtho[1,2-d]thiazol-2-ylamine|||SKA 31|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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