化合物FPTQ T5509

Product Introduction
Bioactivity


英文名: FPTQ

描述: FPTQ，一种mGluR 1的高效拮抗剂，在人类和小鼠mGluR1上展示出6 nM和1.4 nM的IC50值[1]。除了其强大的抑制特性外，FPTQ在体外和体内实验中均表现出显著的抗氧化和抗炎效应[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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.4 mg/mL (14.41 mM)


关键字: FPTQ

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相关库: Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途