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136668-42-3

中文名稱 喹夫拉朋
英文名稱 Quiflapon
CAS 136668-42-3
分子式 C34H35ClN2O3S
分子量 587.18
MOL 文件 136668-42-3.mol
更新日期 2024/11/07 22:55:15
136668-42-3 結(jié)構(gòu)式 136668-42-3 結(jié)構(gòu)式

基本信息

中文別名
喹夫拉朋
英文別名
MK 0591
L-686708
Quiflapon
MK 591(Quiflapon)
MK-0591 (Quiflapon)
QUIFLAPON
MK-591
L-686708
QUIFLAPON
MK0591
MK 0591
3-(3-(tert-Butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylp
3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylMethoxy)-1H-indol-2-yl)-2,2-diMethylpropanoic acid
3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoicaci
所屬類別
醫(yī)藥中間體

物理化學(xué)性質(zhì)

沸點751.3±60.0 °C(Predicted)
密度1.21±0.1 g/cm3(Predicted)
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.70±0.10(Predicted)
形態(tài)粉末
顏色White to off-white

常見問題列表

應(yīng)用
喹夫拉朋可用作醫(yī)藥合成中間體。
生物活性
Quiflapon (MK-591)是一種選擇性和特異性的 FLAP 抑制劑,IC50 為 1.6 nM。Quiflapon 也是一種有效的口服白三烯生物合成 (leukotriene biosynthesis) 抑制劑,在完整的人和誘導(dǎo)的大鼠多形核白細(xì)胞 PMNLs 中,其 IC50 值分別為 3.1 nM 和 6.1 nM。Quiflapon 可以誘導(dǎo)細(xì)胞凋亡 (apoptosis)。
靶點

IC50: 1.6 nM (FLAP).

體外研究

Quiflapon is a potent inhibitor of leukotriene (LT) biosynthesis in intact human and elicited rat polymorphonuclear leukocytes (PMNLs) (IC 50 values 3.1 and 6.1 nM, respectively) and in human, squirrel monkey, and rat whole blood (IC 50 values 510, 69, and 9 nM, respectively). Quiflapon has no effect on rat 5-lipoxygenase. Quiflapon has a high affinity for 5-lipoxygenase activating protein (FLAP) as evidenced by an IC 50 value of 1.6 nM 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.

體內(nèi)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) [1]. Pups were treated with either vehicle or Quiflapon 10, 20, or 40 mg/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.

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