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Bunaprolast

Bunaprolast

产品编号 T17191   CAS 99107-52-5
别名: U66858

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。

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Bunaprolast Chemical Structure
Bunaprolast, CAS 99107-52-5
规格 价格/CNY 货期 数量
1 mg ¥ 4,900 现货
5 mg ¥ 12,600 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Bunaprolast (T17191)
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纯度: 99.9%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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TargetMol Library Books参考文献

1. Johnson HG, et al. Activity of a novel hydroquinone inhibitor of leukotriene synthesis (U-66,858) in the rhesus monkey Ascaris reactor. Int Arch Allergy Appl Immunol. 1988;87(2):204-7. 2. Summers JA, et al. Lipoxygenase inhibitory activity of U-66,858 and its deacetylated metabolite U-68,244 in human whole blood. Agents Actions. 1994 Mar;41(1-2):32-6.
5-Aminosalicylic Acid Isotachioside Psoralidin COX-2/15-LOX-IN-2 1-Naphthyl 3,5-dinitrobenzoate BW 755C COX-2/15-LOX-IN-3 12R-LOX-IN-2

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Keywords

Bunaprolast 99107-52-5 Immunology/Inflammation Metabolism Lipoxygenase LTR U-66858 U 66858 U66858 Inhibitor inhibitor inhibit

 

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