喹夫拉朋
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- CAS号:
- 136668-42-3
- 英文名:
- Quiflapon
- 英文别名:
- MK 0591;L-686708;Quiflapon;MK 591(Quiflapon);MK-0591 (Quiflapon);QUIFLAPON;MK-591;L-686708;QUIFLAPON; MK0591; MK 0591;MK591,FLAP,inhibit,5-LO activating protein,Quiflapon,MK 591,Inhibitor,Apoptosis;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
- 中文名:
- 喹夫拉朋
- 中文别名:
- 喹夫拉朋;1-[(4-氯苯基)甲基]-3-[(1,1-二甲基乙基)硫代]-Α,Α-二甲基-5-(2-喹啉甲氧基)-1H-吲哚-2-丙酸
- CBNumber:
- CB91179632
- 分子式:
- C34H35ClN2O3S
- 分子量:
- 587.17
- MOL File:
- 136668-42-3.mol
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喹夫拉朋化学性质
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沸点:
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751.3±60.0 °C(Predicted)
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密度:
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1.21±0.1 g/cm3(Predicted)
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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酸度系数(pKa):
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4.70±0.10(Predicted)
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喹夫拉朋性质、用途与生产工艺
喹夫拉朋可用作医药合成中间体。
Quiflapon (MK-591)是一种选择性和特异性的 FLAP 抑制剂，IC50 为 1.6 nM。Quiflapon 也是一种有效的口服白三烯生物合成 (leukotriene biosynthesis) 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。Quiflapon 可以诱导细胞凋亡 (apoptosis)。
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.
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.
喹夫拉朋
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-10037 | Quiflapon | | 1 mg | 500元 |
| 2024/04/30 | HY-10037 | 喹夫拉朋
Quiflapon | 136668-42-3 | 5mg | 950元 |
136668-42-3, 喹夫拉朋 相关搜索:
- 药靶配体
- 抑制剂
- C34H35ClN2O3S
- 1-[(4-氯苯基)甲基]-3-[(1,1-二甲基乙基)硫代]-Α,Α-二甲基-5-(2-喹啉甲氧基)-1H-吲哚-2-丙酸
- 喹夫拉朋
- 136668-42-3
- MK591,FLAP,inhibit,5-LO activating protein,Quiflapon,MK 591,Inhibitor,Apoptosis
- 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoicaci
- QUIFLAPON;MK-591;L-686708
- L-686708
- QUIFLAPON; MK0591; MK 0591
- 3-(3-(tert-Butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylp
- MK-0591 (Quiflapon)
- 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-alpha,alpha-dimethyl-5-(2-quinolinylmethoxy)-1H-indole-2-propanoic acid
- MK 591(Quiflapon)
- 1H-Indole-2-propanoic acid, 1-[(4-chlorophenyl)Methyl]-3-[(1,1-diMethylethyl)thio]-α,α-diMethyl-5-(2-quinolinylMethoxy)-
- 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylMethoxy)-1H-indol-2-yl)-2,2-diMethylpropanoic acid
- MK 0591
- Quiflapon