FPTQ 是一种有效的mGluR1拮抗剂,抑制人和鼠的IC50值分别为 6 nM 和 1.4 nM。FPTQ 在体内和体外均具有抗氧化、抗炎作用。
产品描述
FPTQ is potent mGluR 1 antagonist with IC 50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively [1]. FPTQ has anti-oxidant and anti-inflammatory effects both in vitro and in vivo [2].
体外活性
FPTQ (0.5-10 μM) does not shows any cytotoxicity, which 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: RAW264.7 macrophage cells Concentration: 1, 10, or 20 μM Incubation Time: 24 hours Result: Decreased IL-1β and IL-6 mRNA expression
体内活性
Neutrophils translocation in the zebrafish tail-transected model was inhibited by FPTQ. Neutrophil aggregation was also inhibited by FPTQ in the LPS-stimulated zebrafish model. 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].
Cas No.
864863-72-9
分子式
C17H12FN5
分子量
305.31
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years