喹夫拉朋 T16087

Product Introduction
Bioactivity


英文名: Quiflapon

描述: Quiflapon (MK-591) 是一种选择性和特异性的FLAP 抑制剂，可诱导细胞凋亡。它也是口服白三烯生物合成抑制剂，在完整的人和诱导的大鼠多形核白细胞 PMNLs 中，其IC50值分别为 3.1 nM 和 6.1 nM。

体外活性: Quiflapon is an effective inhibitor of leukotriene (LT) biosynthesis in the human, squirrel monkey, and rat whole blood (IC50: 510, 69, and 9 nM, respectively). Quiflapon has a high affinity for 5-lipoxygenase activating protein (FLAP) as evidenced by an IC50 value of 1.6 nM in a FLAP binding assay and inhibition of the photoaffinity labeling of FLAP by two different photoaffinity ligands. However, Quiflapon has no effect on rat 5-lipoxygenase. The inhibition of activation of 5-lipoxygenase was shown through inhibition of the translocation of the enzyme from the cytosol to the membrane in human PMNLs[1].

体内活性: Pups were treated with either vehicle or Quiflapon(10, 20, or 40 mg/kg; daily for days 1-4, 5-9, or 10-14) subcutaneously. On day 14, the lungs were inflated, fixed, and stained for histopathological and morphometric analyses. Inhibition of antigen-induced bronchoconstriction by Quiflapon is observed in inbred rats pretreated with methysergide, Ascaris-challenged squirrel monkeys, and Ascaris-challenged sheep (early and late phase response) [1]. Hyperoxia groups treated with Quiflapon untreated hyperoxia groups displayed definite evidence of aberrant alveolarization but no inflammation[2].

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

溶解度: DMSO : ≥ 50 mg/mL (85.15 mM)
H2O : < 0.1 mg/mL (insoluble)


关键字: MK591 | Quiflapon | FLAP | inhibit | 5-LO activating protein | MK 591 | Inhibitor | Apoptosis

相关产品: Masitinib | APTO-253 | KH16 | PU02 | AES-350 | Glycochenodeoxycholic Acid | Fludarabine Phosphate | Cholesteryl Hemisuccinate | MDK83190 | Glutathione arsenoxide hydrochloride

相关库: ReFRAME Related Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Apoptosis Compound Library | Orally Active Compound 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