| Bioactivity | FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively[1]. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo[2]. | ||||||||||||
| Invitro | 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[2].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[2].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[2]. RT-PCR[1] Cell Line: | ||||||||||||
| In Vivo | 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[2].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[2]. | ||||||||||||
| Name | FPTQ | ||||||||||||
| CAS | 864863-72-9 | ||||||||||||
| Formula | C17H12FN5 | ||||||||||||
| Molar Mass | 305.31 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |