| 产品描述： | FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo |
| 靶点： |
Human mGluR1:6 nM (IC50);Mouse mGluR1:1.4 nM (IC50);GluR |
| 体外研究： |
FPTQ (0.5-10 μM) does not shows any cytotoxicity was not observed at 0.5, 1, 5, and 10 μM in RAW264.7 macrophage cells. FPTQ (1-20 μM; 24 hours) reduces LPS-induced NO production at > 1 μM FPTQ, and at 10 μM, FPTQ treatment causes a 31% anti-oxidant effect in RAW264.7 macrophage cells. FPTQ (1-20 μM; 24 hours) dramaticly decreases LPS-induced expression levels of IL-1β and Il-6. At a concentration of 10 μM, FPTQ causes a 27% and 44% reduction in the mRNA expression of IL-1β and Il-6, respectively in RAW264.7 macrophage cells. RT-PCR Cell Line: RAW264.7 macrophage cells Concentration: 1, 10, or 20 μM Incubation Time: 24 hours Result: Decreased IL-1β and IL-6 mRNA expression |
| 体内研究： |
FPTQ (5-20 μM) decreases the number of neutrophils migrating to the amputation site in zebrafish larvae by tail amputation. In the tailfin wound method, the number of neutrophils collecting at the wound site also decreases in a dose-dependent manner in zebrafish. In a LPS-induced inflammation zebrafish model, LPS solution is injected into the yolks of Tg(mpx:EGFP)i114 zebrafish larvae and exposed the zebrafish larvae immediately to FPTQ treatment. FPTQ (20 μM; 4 hours) significantly decreases the fluorescent neutrophils after yolk injection and has an anti-inflammatory effect during the early phase of inflammation |
| 参考文献： |
1. Fujinaga M et al. Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain. Bioorg Med Chem, 2011 Jan 1, 19(1):102 2. Geum Ran Kim, et al. Anti-inflammatory effect of a novel synthetic compound 1-((4-fluorophenyl)thio)isoquinoline in RAW264.7 macrophages and a zebrafish model. Fish Shellfish Immunol. 2019 Apr;87:395-400. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.275 ml |
16.377 ml |
32.754 ml |
| 5 mM |
0.655 ml |
3.275 ml |
6.551 ml |
| 10 mM |
0.328 ml |
1.638 ml |
3.275 ml |
| 50 mM |
0.066 ml |
0.328 ml |
0.655 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京