Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels.
产品描述 | GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels. |
靶点活性 | TRPC6 (rat):4 nM (IC50), TRPC3 (rat):5 nM (IC50) |
体外活性 | Nuclear factor of activated T cells (NFAT) activation by Ang II ( angiotensin II) is blocked in a dose dependent manner by GSK255B (0.01, 0.1, and 1 μM) in HEK293T cells overexpressing TRPC3. GSK255B blocks NFAT activation by Ang II in HEK293T cells expressing a mutant TRPC6 channel with T70 and S322 mutated to glutamic acid (SETE)[1]. GSK255B (10 μM) blocks calcium entry stimulated by Phenylephrine (20 μM) in rat neonatal cardiac myocytes. GSK255B dose-dependent blockade of cell hypertrophy signaling triggered by angiotensin II or endothelin-1 in HEK293T cells as well as in neonatal and adult cardiac myocytes[1]. |
分子量 | 411.88 |
分子式 | C18H19ClFN3O3S |
CAS No. | 1366233-41-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
GSK2332255B 1366233-41-1 GSK-2332255B Inhibitor inhibitor inhibit