| Description | FPTQ is a highly effective antagonist of mGluR 1, displaying IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively [1]. In addition to its robust inhibitory properties, FPTQ exhibits notable antioxidant and anti-inflammatory effects in both in vitro and in vivo settings [2]. |
| In vitro | FPTQ（0.5-10μM）在RAW264.7巨噬细胞中未显示任何细胞毒性，该现象在0.5、1、5和10μM的浓度下均未观察到[2]。FPTQ（1-20μM；24小时）在大于1μM的浓度下减少了LPS诱导的NO产生，在10μM浓度下，FPTQ治疗显示了31%的抗氧化效果[2]。FPTQ（1-20μM；24小时）显著降低了LPS诱导的IL-1β和Il-6的表达水平，在10μM浓度下，FPTQ分别使IL-1β和Il-6 mRNA的表达量降低了27%和44%[2]。采用RT-PCR方法[1]，细胞系为RAW264.7巨噬细胞，浓度为1、10或20μM，孵育时间为24小时，结果显示IL-1β和IL-6 mRNA表达降低。 |
| In vivo | 在斑马鱼尾部切除模型中，FPTQ抑制了中性粒细胞的转移。在LPS刺激的斑马鱼模型中，FPTQ也抑制了中性粒细胞的聚集。FPTQ（5-20 μM）通过尾部截肢减少了迁移到切口位置的中性粒细胞数量。在尾鳍创伤方法中，中性粒细胞在创伤部位聚集的数量也表现出剂量依赖性的减少[2]。在LPS诱导的炎症斑马鱼模型中，将LPS溶液注射到Tg(mpx:EGFP) i114斑马鱼幼鱼的卵黄中，并立即将斑马鱼幼鱼暴露于FPTQ处理。FPTQ（20 μM；4小时）显著减少了卵黄注射后的荧光中性粒细胞，并在炎症初期阶段表现出抗炎效果[2]。 |
| molecular weight | 305.31 |
| Molecular formula | C17H12FN5 |
| CAS | 864863-72-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.4 mg/mL (14.41 mM) |
| References | 1. Geum Ran Kim, Jung Yoon Yang, Kyu-Seok Hwang,et al. Anti-inflammatory effect of a novel synthetic compound 1-((4-fluorophenyl)thio)isoquinoline in RAW264.7 macrophages and a zebrafish model.[J]. Fish & shellfish immunology, 2019. |