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包装规格:1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(≥ 50 mg/mL)
产品描述:基本信息 产品编号:Q10041  产品名称:Quiflapon CAS: 136668-42-3   储存条件 粉末 -20℃ 四年     分子式: C34H35ClN2O3S 溶于液体 -80℃ 六个月 分子量 587.17 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.7031mL 8.5154mL 17.0308mL 5mM 0.3406mL 1.7031mL 3.4062mL 10mM 0.1703mL 0.8515mL 1.7031mL   生物活性 产品描述 一种选择性和特异性的 FLAP 抑制剂,IC50 为 1.6nM。 靶点/IC50 1.6nM (FLAP)   体外研究 Quiflapon is a potent inhibitor of leukotriene (LT) biosynthesis in intact human and elicited rat polymorphonuclear leukocytes (PMNLs) (IC50 values 3.1 and 6.1nM,respectively) and in human,squirrel monkey, and rat whole blood (IC50 values 510, 69, and 9nM,respectively).Quiflapon has no effect on rat 5-lipoxygenase. Quiflapon has a high affinity for 5-lipoxygenase activating protein (FLAP) as evidenced by an IC50 value of 1.6nM in a FLAP binding assay and inhibition of the photoaffinity labelling of FLAP by two different photoaffinity ligands. 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. 体内研究 Quiflapon is a potent inhibitor of LT biosynthesis in vivo, first, following ex vivo challenge of blood obtained from treated rats and squirrel monkeys, second, in a rat pleurisy model, and, third, as monitored by inhibition of the urinary excretion of LTE4 in antigen-challenged allergic sheep.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). Pups were treated with either vehicle or Quiflapon 10, 20, or 40mg/kg subcutaneously daily for days 1-4, 5-9, or 10-14. On day 14, the lungs were inflated,fixed, and stained for histopathological and morphometric analyses. Hyperoxia groups treated with Quiflapon untreated hyperoxia groups showed definite evidence of aberrant alveolarization but no inflammation.
保存条件:-20℃