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包装规格：100mg 250mg 1g in glass bottle
产品简介：一种有效的DHODH抑制剂。
溶解性：溶于DMSO
储备液保存：-80°C, 1 years -20°C, 6 months
体内实验：1、请依序添加每种溶剂： 10% DMSO→ 40% PEG300 →5% Tween-80 →45% Saline Solubility: 2.08 mg/mL (5.54 mM); 悬浊液; 超声加热助溶 此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。 2、请依序添加每种溶剂： 10% DMSO → 90% Corn Oil Solubility: ≥ 2.08 mg/mL (5.54 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
靶点：DHODH 20 nM
体外研究：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 p56lck 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 p56lck 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 p59fyn 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 p59fyn 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.
体内研究：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.
保存条件：-20℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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