Quiflapon sodium (Synonyms: MK-591 sodium)
目录号: PL05083 纯度: ≥99%
CAS No. :147030-01-1
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中文名称
Quiflapon sodium
中文别名
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-丙酸钠;喹夫拉朋钠;1-[(4-氯苯基)甲基]-3-[(1,1-二甲基乙基)硫代]-Alpha,Alpha-二甲基-5-(2-喹啉甲氧基)-1H-吲哚-2-丙酸钠
英文名称
Quiflapon sodium
英文别名
1H-Indole-2-propanoicacid, 1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-a,a-dimethyl-5-(2-quinolinylmethoxy)-, sodium salt (1:1);Quiflapon Sodium;MK591;1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(2-quinolinylmethoxy)-1H-Indole-2-propanoic acid sodium salt;1H-Indole-2-propanoicacid, 1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-a,a-dimethyl...;1H-Indole-2-propanoicacid, 1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-a,a-dimethyl-5-(2-quinolinylmethoxy)-, sodi;sodium,3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoate;MK-591;sodium 3-[1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)-3-tert-butylsulfanyl-indol-2-yl]-2,2-dimethyl-propanoate;MK 591
Cas No.
147030-01-1
分子式
C34H34N2O3Scl-.Na+
分子量
609.15
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Quiflapon sodium (MK-591 sodium) 是选择性的,特异性的 FLAP 抑制剂。Quiflapon sodium 是一种有效的,具有口服活性的白三烯生物合成 (leukotriene biosynthesis) 抑制剂。诱导细胞凋亡 (apoptosis)。
生物活性
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
性状
Solid
体外研究(In Vitro)
Quiflapon sodium (MK591) and SB203580 are able to block SEB-induced human PBMC cell proliferation. Quiflapon sodium (MK591) down regulates three genes [for cathepsin L, IL-17 and guanylate binding protein (GBP)-2] that are up regulated by SEB. Quiflapon sodium (MK591) undergoes apoptosis within hours of treatment. Quiflapon sodium also induces rapid activation of the stress kinase, c-Jun N-terminal kinase (JNK), which plays an important role in the apoptosis process. Quiflapon sodium triggers apoptosis in prostate cancer cells without inhibition of PI3K-Akt, or ERK. Moreover, Quiflapon sodium and LY294002 exert synergistic effect in inducing apoptosis in prostate cancer cells. Quiflapon sodium (MK591) influences cAMP response element-binding protein but not Sp1. has not independently confirmed the accuracy of these meth
体内研究(In Vivo)
Hyperoxia groups of mice treated with Quiflapon sodium (MK591) (20, 40 mg/kg) show alveolarization that resembles that of room air controls while untreated hyperoxia groups show definite evidence of aberrant alveolarization but no inflammation. Comparison of the Aβ-immunopositive areas between the placebo and Quiflapon sodium (MK591) (320 mg/kg)-treated group reveals a statistically significant reduction of the amyloid burden in the treated mice. Quiflapon sodium also has a significant reduction in brain levels of IL-1β. Mice treated with Quiflapon sodium show a statistically significant decrease in the steady-state levels of total CREB and its phosphorylated form at Ser133. 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
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Mendis C, et al. Effect of 5-lipoxygenase inhibitor MK591 on early molecular and signaling events induced by staphylococcal enterotoxin B in human peripheral blood mononuclear cells. FEBS J. 2008 Jun;275(12):3088-98.
[2]. Sarveswaran S, et al. MK591, a leukotriene biosynthesis inhibitor, induces apoptosis in prostate cancer cells: synergistic action with LY294002, an inhibitor of phosphatidylinositol 3-kinase. Cancer Lett. 2010 May 28;291(2):167-76.
溶解度数据
In Vitro: DMSO : 50 mg/mL (82.08 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液
搜索质检报告(COA)

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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