store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bunaprolast (U66858) 是一种新型有效的白三烯 B4 (LTB4) 抑制剂。Bunaprolast 具有氧化降解活性,对脂氧合酶 (lipoxygenase)和 TXB2 释放具有抑制作用。
产品描述 | Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release. |
靶点活性 | LTB4:250±85 nM |
体外活性 | Bunaprolast (U-66,858) undergoes deacetylation to an initial metabolite with similar pharmacological potency. The inhibitory effects of the semi-quinone Bunaprolast and its metabolite U-68,244 on the ionophore-induced formation of leukotriene B4 (LTB4) are examined in human whole blood (WB). Preincubation of Bunaprolast and U-68,244 for 1 min prior to the challenge of blood with calcium ionophore A23187 results in IC50s of 1080±644 and 820±442 nM, respectively. After 60 min preincubation, IC50s are 250±85 and 270±79 nM. The activity of the lipoxygenase inhibitor AA-861 in this system is similar to that of Bunaprolast, while vitamin K and the sulfate conjugate of Bunaprolast show significant inhibition of LTB4 release only at micromolar concentrations. Bunaprolast exhibits significant inhibition of thromboxane A2 release (p<0.02) in a comparative study with the known cyclooxygenase (CO) inhibitor Flurbiprofen[2]. |
体内活性 | The IgE-mediated hypersensitivity to Ascaris antigen in reactor rhesus primates is used to assess the pharmacologic profile of Bunaprolast (U-66,858). When given orally, Bunaprolast shows dose-related inhibition of resistance (RL) and compliance (Cdyn) changes. When administered via aerosol, it exhibits dose-independent inhibition. In 15 animals receiving aerosols (52±32 to 53±10% for RL, p=0.05, and 45±19 to 28±19% Cdyn inhibitions, p=0.05) at concentrations ranging from 5.0% to 0.1%, Bunaprolast demonstrates significant effects. By the oral route, inhibition is observed at 1-4 h following administration. In 5 animals, oral doses of 10 and 5 mg/kg result in inhibition (RL by 98±2 to 78±1.5%, p=0.01, and Cdyn by 75±17 to 60.9±9.1%, p=0.05) for 10 and 5 mg/kg of Bunaprolast, respectively[1]. |
别名 | U66858 |
分子量 | 272.34 |
分子式 | C17H20O3 |
CAS No. | 99107-52-5 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Bunaprolast 99107-52-5 Immunology/Inflammation Metabolism Lipoxygenase LTR U-66858 U 66858 U66858 Inhibitor inhibitor inhibit