PF-4191834 (Synonyms: PF-04191834)
目录号: PL06746 纯度: ≥99%
CAS No. :1029317-21-2
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中文名称
PF-4191834
中文别名
4-[3-[4-(2-methylpyrazol-3-yl)phenyl]sulfanylphenyl]oxane-4-carboxamide
英文名称
PF-4191834
英文别名
4-(3-(4-(1-Methyl-1H-pyrazol-5-yl) phenylthio) phenyl)-tetrahydro-2H-pyran-4-carboxamide;PF 4191834;Tetrahydro-4-[3-[[4-(1-methyl-1H-pyrazol-5-yl)phenyl]thio]phenyl]-2H-pyran-4-carboxamide;PF-4191834;YX55DXP4T1;4-(3-(4-(1-methyl-1H-pyrazol-5-yl)phenylthio)phenyl)-tetrahydro-2H-pyran-4-carboxamide;4-[3-[4-(2-methylpyrazol-3-yl)phenyl]sulfanylphenyl]oxane-4-carboxamide;4-(3-((4-(1-methyl-1H-pyrazol-5-yl)phenyl)thio)phenyl)tetrahydro-2H-pyran-4-carboxamide;PF 04191834;GTPL9054;DB11645;SB19645;PF04191834;Q27088313;4-(3-{[4-(1-methyl-1H-p
Cas No.
1029317-21-2
分子式
C22H23N3O2S
分子量
393.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-4191834 (PF-04191834) 是一种具有口服活性的,非铁螯合的,非氧化还原的 5-脂氧合酶 (5-LOX) 抑制剂(IC50=229 nM),PF-4191834 对 5-LOX 的选择性约是 12-LOX 和 15-LOX 的 300 倍,对环氧合酶没有活性,对炎症和疼痛有效。
生物活性
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC 50 =229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
性状
Solid
IC50 & Target[1][2]
5-LOX
体外研究(In Vitro)
PF-4191834 (PF-04191834) inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC50 values between 100 and 190 nM and do not inhibit significantly the COX-1/2 enzymes or the 12- or 15-LOX enzymes at concentrations up to 30 μM.
PF-4191834 (PF-04191834) exerts a concentration-dependent inhibition of human 5-LOX, with an IC50 value of 130 nM and an IC80 value of 370 nM. 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
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Masferrer JL, et al. Pharmacology of PF-4191834, a novel, selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. J Pharmacol Exp Ther. 2010 Jul;334(1):294-301.
溶解度数据
In Vitro: DMSO : 100 mg/mL (254.13 mM; Need ultrasonic)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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