Nabumetone
(Synonyms: 萘丁美酮; BRL14777) 目录号 : GC13422
An NSAID and a prodrug form of 6-methoxy naphthalene acetic acid
Cas No.:42924-53-8
Sample solution is provided at 25 µL, 10mM.
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Nabumetone is a potent and selective COX-2 inhibitor. Nabumetone (50 μmol-2 mmol) dose-dependently inhibits the proliferation of K-562 and Meg-01 cells, but shows no obvious apoptotic effect. Nabumetone potentiates the apoptotic effect of ADR in the K-562 cell line. Moreover, Nabumetone reduces Bcl-2 expression[1].
Nabumetone (79 mg/kg, p.o.) inhibits paw oedema and paw exudate PGE2 in rats. Nabumetone does not induce gastric damage and causes only 57% inhibition of gastric mucosal 6-keto-PGF1α production in rats[2]. Nabumetone (25, 50, 100 mg/kg, i.p.) dose-dependently inhibits the increase of DDC-induced mucus secretion and stimulates stress-induced mucus secretion in rats. Nabumetone (25 mg/kg, i.p.) significantly suppresses stress-induced ulcer index in rats[3].
Reference：
[1]. Vural F, et al. Cyclo-oxygenase 2 inhibitor, nabumetone, inhibits proliferation in chronic myeloid leukemia cell lines. Leuk Lymphoma. 2005 May;46(5):753-6.
[2]. Melarange R, et al. Anti-inflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6MNA (6-methoxy-2-naphthylacetic acid): comparison with indomethacin. Agents Actions. 1992;Spec No:C82-3.
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Cell experiment: |
Every cell line is plated into 6-well plates at a concentration of 3 × 105/mL with or without drugs (Nabumetone, etc.) and incubated for 48 h. Viable cells are then counted using the trypan blue dye exclusion test. The percentage of proliferation inhibition is calculated as 1-(viable cells exposed to drug/viable cells in control) ×100[1]. |
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Animal experiment: |
Rats[3]Albino male rats (250- to 300-g body weight) are used in the study. The animals are maintained in a single cage and are deprived of food for 16 h before the onset of experiments. Free access to water is allowed until 1 h before the beginning of experiments. There are eight rats in each group. The animals are pretreated with intraperitoneal injections of Nabumetone or dipyrone at 25-, 50-, or 100-mg/kg doses for 3 days[3]. |
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References: [1]. Vural F, et al. Cyclo-oxygenase 2 inhibitor, nabumetone, inhibits proliferation in chronic myeloid leukemia cell lines. Leuk Lymphoma. 2005 May;46(5):753-6. |
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| Cas No. | 42924-53-8 | SDF | |
| 别名 | 萘丁美酮; BRL14777 | ||
| 化学名 | 4-(6-methoxynaphthalen-2-yl)butan-2-one | ||
| Canonical SMILES | CC(=O)CCC1=CC2=C(C=C1)C=C(C=C2)OC | ||
| 分子式 | C15H16O2 | 分子量 | 228.29 |
| 溶解度 | ≥ 11.4mg/mL in DMSO | 储存条件 | Store at 2-8°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 | 4.3804 mL | 21.902 mL | 43.8039 mL |
| 5 mM | 0.8761 mL | 4.3804 mL | 8.7608 mL |
| 10 mM | 0.438 mL | 2.1902 mL | 4.3804 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet