store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK1016790A (GSK101) 是选择性瞬时受体电位香草酸 4 通道激活剂,可引起 HEK 细胞中 Ca2+流入并升高细胞内 Ca2+。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 2,950 | 现货 | ||
100 mg | ¥ 4,350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 795 | 现货 |
产品描述 | GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells. |
靶点活性 | TRPV4:34 nM(EC50) |
体外活性 | GSK1016790A elicits Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM[1]. It stimulates TRPV4 in multiple cell types including endothelial cells, urinary smooth muscle cells, urothelial cells and HEK-293 cells over-expressing TRPV4. GSK1016790A specifically activates TRPV4 channels, leading to a rapid partial desensitization and downregulation of the channel expression on the plasma membrane[2]. |
体内活性 | GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions[3]. The activation of TRPV4 by GSK1016780A leads to vasodilation, vascular leakage, and tissue hemorrhage[4]. |
细胞实验 | CPECs are treated for 20 minutes with vehicle(DMSO), 10 nM GSK, or 10 nM GSK following the pretreatment with 1 mM HC. Then the cells are fixed and stained with Coomassie Brilliant Blue.(Only for Reference) |
别名 | GSK101 |
分子量 | 655.61 |
分子式 | C28H32Cl2N4O6S2 |
CAS No. | 942206-85-1 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 58 mg/mL(88.5 mM)
DMSO: 93 mg/mL (141.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.5253 mL | 7.6265 mL | 15.253 mL | 38.1324 mL |
5 mM | 0.3051 mL | 1.5253 mL | 3.0506 mL | 7.6265 mL | |
10 mM | 0.1525 mL | 0.7626 mL | 1.5253 mL | 3.8132 mL | |
20 mM | 0.0763 mL | 0.3813 mL | 0.7626 mL | 1.9066 mL | |
50 mM | 0.0305 mL | 0.1525 mL | 0.3051 mL | 0.7626 mL | |
DMSO | 100 mM | 0.0153 mL | 0.0763 mL | 0.1525 mL | 0.3813 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。
GSK1016790A 942206-85-1 Membrane transporter/Ion channel Metabolism Calcium Channel TRP/TRPV Channel inhibit Ca2+ channels Inhibitor embryonic GSK-101 GSK-1016790A Ca channels HEK vanilloid transient potential receptor GSK 101 TRP Channel kidney GSK101 human Transient receptor potential channels inhibitor