Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronchoconstriction.
产品描述 | GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronchoconstriction. |
靶点活性 | NK2:10 (pki)( Rat colon membrane), NK2 (human):9.51(pki) (CHO cell) |
体外活性 | GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM, and 4T1 cells) treatment enhances phosphorylation of P38. At the same time, it also inhibiting AKT activation in all metastatic cell lines whereas phosphorylation of ERK decreased in 4TBM, 4TLM, and 4THM but not in 4T1 cells. GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM, and 67NR cells) treatment inhibits proliferation of cells in all cell lines dose-dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells [2]. |
体内活性 | GR 159897 (0.12 mg/kg; i.v.; guinea-pigs) treatment effectively antagonizes bronchoconstriction caused by GR64349. It has a long duration of action (3 h) [1]. |
分子量 | 414.54 |
分子式 | C23H27FN2O2S |
CAS No. | 158848-32-9 |
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。
GR 159897 158848-32-9 Others GR159897 GR-159897 Inhibitor inhibitor inhibit