FPTQ
目录号: PL07139 纯度: ≥99%
CAS No. :864863-72-9
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中文名称
FPTQ
中文别名
FPTQ
英文名称
FPTQ
英文别名
FPTQ;6-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]quinoline;Quinoline, 6-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-
Cas No.
864863-72-9
分子式
C17H12FN5
分子量
305.31
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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 具有抗氧化、抗炎作用。
生物活性
FPTQ is potent mGluR 1 antagonist with IC 50 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.
性状
Solid
IC50 & Target[1][2]
Human mGluR1 6 nM (IC50) Mouse mGluR1 1.4
体外研究(In Vitro)
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
In a LPS-induced inflammation zebrafish model, LPS solution is injected into the yolks of Tg(mpx:EGFP) 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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (109.17 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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