Brequinar|96187-53-0|(DUP785; NSC 368390)-陌孚医药/Medlife

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Brequinar (Synonyms: DUP785; NSC 368390)

目录号: PL01668 纯度: ≥99%

CAS No. :96187-53-0

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中文名称	Brequinar
中文别名	布喹那;6-氟-2-(2’-氟联苯-4-基)-3-甲基喹啉-4-羧酸;6-氟-2-(2'-氟-[1,1'-联苯]-4-基)-3-甲基喹啉-4-羧酸
英文名称	Brequinar
英文别名	6-Fluoro-2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid;6-fluoro-2-(2'-fluorobiphenyl-4-yl)-3-methylquinoline-4-carboxylic acid;6-fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methylquinoline-4-carboxylic acid;Brequinar;Brequinar [INN];brequinar potassium;BREQUINAR SODIUM;Brequinarum [INN-Latin];brequinarum [Latin];Dup 785;BPQ;Biphenquinate;6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid;C23H15F2NO2;PHEZJEYUWHETKO-UHFFFAOYSA-N;5XL19F49H6;6-FLUORO-2-(2'-FLUORO-1,1'-BIPHENYL-4-YL)-3-METHYLQUINOLINE-4-CARBOXYLIC ACID;breq;6-Fluoro-2-(2′-fluoro[1,1′-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid (ACI)
Cas No.	96187-53-0
分子式	C₂₃H₁₅F₂NO₂
分子量	375.37
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Brequinar (DUP785) 是一种有效的 dihydroorotate dehydrogenase (DHODH) 抑制剂，对人的 IC₅₀ 值为 5.2 nM，也是一种广谱的抗病毒剂，同时具有抗 SARS2 的活性。

生物活性

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC 50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

性状

Solid

体外研究(In Vitro)

Brequinar reduces virus progeny production by >90%, with EC50 of 17 nM. Brequinar (5?μM) also inhibits other orthopoxviruses, and blocks virus DNA replication. Brequinar does not affect virus early gene expression, but has a severe effect on the late stage of the virus cycle. Brequinar reduces the level of envelope protein production and the viral titer in a dose-dependent manner, with EC50 of 78 nM in the CFI assay. Brequinar (5 μM) inhibits viral RNA synthesis. Brequinar has antiviral effect, but the effect is reversed by pyrimidine. Brequinar-resistant viruses can be selected in cell culture. Brequinar (5 μM) suppresses the luciferase activities from both the WT and NS5 mutant replicons. Brequinar sodium effectively prevents the increase in PyNTP levels with an IC50 of 0.26 μM. Brequinar sodium effectively inhibits cell proliferation with

体内研究(In Vivo)

Brequinar sodium-treated (10-20 mg/kg/day) mice has a 31% reduction in percentage of packed cell volume compared with untreated BALB/c mice. Brequinar sodium reduces UTP and CTP levels in bone marrow cells by 30 and 25%, respectively. Brequinar sodium (10-20 mg/kg/day) in combination with uridine (1000-2000 mg/kg/day) prevents anemia, and the hematocrits remain at levels (61-63%) comparable with those of untreated controls. 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]. Schnellrath LC, et al. Potent antiviral activity of brequinar against the emerging Cantagalo virus in cell culture. Int J Antimicrob Agents. 2011 Nov;38(5):435-41.
[2]. Qing M, et al. Characterization of dengue virus resistance to brequinar in cell culture. Antimicrob Agents Chemother. 2010 Sep;54(9):3686-95.

溶解度数据	In Vitro: DMSO : 25 mg/mL (66.60 mM; Need ultrasonic)配制储备液

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Data Sheet

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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