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