Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂,也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流,延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 498 | 现货 | ||
10 mg | ¥ 713 | 现货 | ||
25 mg | ¥ 1,470 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,330 | 现货 | ||
200 mg | ¥ 6,180 | 现货 | ||
500 mg | ¥ 9,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 589 | 现货 |
产品描述 | SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ/AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner. |
体外活性 | SKF-96365 exhibits protective activity against MPP+ injury in PC12 cells and significantly inhibits apoptotic cell death in PC12 cells after MPP+ administration. SKF-96365 does not exert effects on necrotic cell death induced by MPP+ insult in PC12 cells. Because of its non-selective activity, SKF-96365 has been demonstrated to have effects on multiple other Ca2+ channels: it not only blocks high-voltage-activated (HVA) Ca2+ channels at typically utilized test concentrations, but also potently inhibits low-voltage -activated (LVA) T-type Ca2+ channels in HEK293 cells. The exact effect of SKF-96365 on intracellular calcium homeostasis might dependent on cell types and experimental models used[2]. |
体内活性 | SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo[4]. |
细胞实验 | To investigate whether SKF-96365 could protect PC12 cells from injury induced by MPP+ insult, cultured PC12 cells are pretreated with SKF-96365 in different concentrations (1 µM, 10 µM or 50 µM) 30 min before MPP+ addition. The cells viability is measured 24 h after MPP+ insult by using the cell proliferation reagent WST-1. (Only for Reference) |
别名 | 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑, SKF96365 |
分子量 | 402.91 |
分子式 | C22H27ClN2O3 |
CAS No. | 130495-35-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 198.6 mM
H2O: 198.6 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.4819 mL | 12.4097 mL | 24.8194 mL | 62.0486 mL |
5 mM | 0.4964 mL | 2.4819 mL | 4.9639 mL | 12.4097 mL | |
10 mM | 0.2482 mL | 1.241 mL | 2.4819 mL | 6.2049 mL | |
20 mM | 0.1241 mL | 0.6205 mL | 1.241 mL | 3.1024 mL | |
50 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.241 mL | |
100 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6205 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。
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