BW 755C
目录号 : GC14601
Dual 5-LO/COX inhibitor
Cas No.:66000-40-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml for 5-LO, COX-1, and COX-2, respectively
BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways.
Constitutive cyclooxygenase (COX-1) is present in cells under physiological conditions, whereas COX-2 is induced by some cytokines, mitogens, and endotoxin in pathological conditions, such as inflammation. Since 5-lipoxygenase (5-LO) oxidizes arachidonic acid to 5-hydroperoxyeicosatetraenoic acid in the first step of the leukotriene pathway, 5-LO inhibitors should prevent leukotriene biosynthesis and thus prove useful in the treatment of allergic asthma.
In vitro: Previous study found that BW 755C and other nonsteroidal antiinflammatory drugs including diclofenac, acetaminophen, and naproxen showed approximately equipotent inhibitory effects on COX-1 and COX-2 in intact cells. Whereas, BF 389 was the most potent and most selective inhibitor of COX-2 in intact cells [1].
In vivo: An animal study was conducted to examine whether BW-755C delayed neuronal death in the hippocampal CA1 sector in Mongolian gerbils after 5 minutes of forebrain ischemia. Gerbils were injected with BW-755C. Seven days after ischemic insult, the animals were perfusion-fixed, and the neuronal density in the hippocampal CA, sector was estimated. Results showed that in ischemic gerbils with vehicle administration, the average neuronal density was 13 for BW-755C. In ischemic gerbils treated with 30 mg/kg BW-755C, the average neuronal densities was 14 [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Mitchell, J. A.,Akarasereenont, P.,Thiemermann, C., et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proceedings of the National Academy of Sciences of the United States of America 90, 11693-11697 (1993).
[2] Nakagomi T, Sasaki T, Kirino T, Tamura A, Noguchi M, Saito I, Takakura K. Effect of cyclooxygenase and lipoxygenase inhibitors on delayed neuronal death in the gerbil hippocampus. Stroke. 1989 Jul;20(7):925-9.
| Cas No. | 66000-40-6 | SDF | |
| 化学名 | 4,5-dihydro-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-3-amine | ||
| Canonical SMILES | NC(CC1)=NN1C2=CC=CC(C(F)(F)F)=C2 | ||
| 分子式 | C10H10F3N3 | 分子量 | 229.3 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;25mg/ml in dimethyl formamide | 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 | 4.3611 mL | 21.8055 mL | 43.611 mL |
| 5 mM | 0.8722 mL | 4.3611 mL | 8.7222 mL |
| 10 mM | 0.4361 mL | 2.1805 mL | 4.3611 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。