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萘丁美酮 /Nabumetone {[allProObj[0].p_purity_real_show]}

货号:A307752 同义名: BRL14777

Nabumetone is a non-steroidal anti-inflammatory drug (NSAID) and its active metabolite inhibits the COX.

Nabumetone 化学结构 CAS号:42924-53-8
Nabumetone 化学结构
CAS号:42924-53-8
Nabumetone 3D分子结构
CAS号:42924-53-8
Nabumetone 化学结构 CAS号:42924-53-8
Nabumetone 3D分子结构 CAS号:42924-53-8
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Nabumetone 纯度/质量文件 产品仅供科研

货号:A307752 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 99%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Rofecoxib ++++

COX-2, IC50: 18 nM

98%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

98%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

98%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Nabumetone 生物活性

靶点
  • COX

描述 Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA. 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 (Adriamycin) in the K-562 cell line. Moreover, Nabumetone reduces Bcl-2 expression[3]. An oral dose of nabumetone (79 mg/kg) or intravenous 6MNA produced effective anti-inflammatory activity together with significant inhibition of paw exudate PGE2. An anti-inflammatory oral dose of nabumetone or intravenous 6MNA produced minimal effects on gastric 6-keto-PGF1 alpha production, with an absence of gastric damage, in contrast to indomethacin[4]. When compared with currently available NSAIDs, nabumetone may be associated with a significantly lower incidence of gastroduodenal ulcer, and that nabumetone also appears to be safer for use in elderly patients and in those with renal or hepatic impairment[5].

Nabumetone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01638962 Osteoarthritis, Knee Not Applicable Completed - Denmark ... 展开 >> University of Southern Denmark Odense, Region Syddanmark, Denmark, 5230 收起 <<
NCT01761864 Study Focus: Prescribing of Dr... 展开 >>ugs 收起 << Not Applicable Unknown January 2016 Belgium ... 展开 >> University of Antwerp Wilrijk, Belgium, 2610 收起 <<
NCT00363532 Migraine Without Aura Not Applicable Completed - Denmark ... 展开 >> Danish Headache Center, Neurological Dep. Glostrup hospital Glostrup, Denmark, 2770 收起 <<

Nabumetone 参考文献

[1]Hedner T, Samulesson O, et al. Nabumetone: therapeutic use and safety profile in the management of osteoarthritis and rheumatoid arthritis. Drugs. 2004;64(20):2315-43; discussion 2344-5.

[2]Boyle EA, Freeman PC, et al. Nabumetone (BRL 14777, 4-[6-methoxy-2-naphthyl] -butan-2-one): a new anti-inflammatory agent. J Pharm Pharmacol. 1982 Sep;34(9):562-9.

[3]Vural F, Ozcan MA, Ozsan GH, Ateş H, Demirkan F, Pişkin O, Undar B. Cyclo-oxygenase 2 inhibitor, nabumetone, inhibits proliferation in chronic myeloid leukemia cell lines. Leuk Lymphoma. 2005 May;46(5):753-6

[4]Melarange R, Gentry C, O'Connell C, Blower PR, Neil C, Kelvin AS, Toseland CD. 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

[5]Roth SH. Nabumetone: a new NSAID for rheumatoid arthritis and osteoarthritis. Orthop Rev. 1992 Feb;21(2):223-7

Nabumetone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.38mL

0.88mL

0.44mL

21.90mL

4.38mL

2.19mL

43.80mL

8.76mL

4.38mL

Nabumetone 技术信息

CAS号42924-53-8
分子式C15H16O2
分子量 228.286
别名 BRL14777
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(459.95 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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