Bunaprolast (U66858)
(Synonyms: 布那司特,U66858) 目录号 : GC32002
Bunaprolast (U66858) (U66858) 是人类全血中产生 LTB4 的有效抑制剂。
Cas No.:99107-52-5
Sample solution is provided at 25 µL, 10mM.
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Bunaprolast (U66858) is a potent inhibitor of LTB4 production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB2 release.
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 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 sulphate conjugate of Bunaprolast show significant inhibition of LTB4 release only at micromolar concentrations. Bunaprolast exhibits significant inhibition of thromboxane A2 release (p
The IgE-mediated hypersensitivity to Ascaris antigen in reactor rhesus primates is used to assess the pharmacologic profile of Bunaprolast (U-66,858). When Bunaprolast is given by the oral route, it shows dose-related inhibition of resistance (RL) and compliance (Cdyn) changes. When Bunaprolast is given by the aerosol route, it shows dose independent inhibition. In 15 animals, aerosols (52±32 to 53±10% for RL, p=0.05 and 45±19 to 28±19% Cdyn inhibitions, p=0.05) for 5.0-0.1% aerosol. By the oral route, inhibition is seen at 1-4 h following administration. In 5 animals, oral doses of 10 and 5 mg/kg inhibit (RL by 98±2 to 78±1.5%, p=0.01 and Cdyn by 75±17 to 60.9±9.1%, p=0.05) by 10 and 5 mg/kg Bunaprolast, respectively[2].
[1]. 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. [2]. 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.
| Cas No. | 99107-52-5 | SDF | |
| 别名 | 布那司特,U66858 | ||
| Canonical SMILES | COC1=C2C=CC=CC2=C(OC(C)=O)C(CCCC)=C1 | ||
| 分子式 | C17H20O3 | 分子量 | 272.34 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6719 mL | 18.3594 mL | 36.7188 mL |
| 5 mM | 0.7344 mL | 3.6719 mL | 7.3438 mL |
| 10 mM | 0.3672 mL | 1.8359 mL | 3.6719 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet