Brequinar

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Brequinar

CAS No. : 96187-53-0

MCE 国际站：Brequinar

产品活性：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。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection  |  Cell Cycle/DNA Damage

作用靶点：Dihydroorotate Dehydrogenase  |  SARS-CoV  |  Virus Protease  |  DNA/RNA Synthesis

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 an IC₅₀ of 0.26 μM. Brequinar sodium inhibits autophosphorylation of p56^lck with IC₅₀ of 70 μM; inhibition is 39, 41, and 60% for 25, 50, and 100 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p56^lck of the exogenous substrate, histone 2B, with an IC₅₀ of 70 μM; inhibition is 10, 43, 59, and 86% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium inhibits autophosphorylation of p59^fyn with an IC₅₀ of 105 μM; inhibition is 0, 17, 48, and 65% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p59^fyn of histone 2B with an IC₅₀ of 20 μM; inhibition is 26, 54, 79, 83, and 84% for 10, 25, 50, 100, and 200 μM Brequinar sodium, respectively.

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.

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