| Name | Nabumetone |
| Description | Nabumetone (BRL14777)(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite 6MNA inhibits the enzymes cyclo-oxygenase I and II. |
| Kinase Assay | Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay. |
| In vitro | Nabumetone exhibits anti-inflammatory activity in rat models of carrageenan-induced edema and UV-induced erythema in guinea pigs. In a rat granuloma model, Nabumetone is non-toxic at concentrations higher than the minimum effective dose. Furthermore, in adjuvant-induced arthritic rats, Nabumetone demonstrates good gastric tolerability at doses exceeding those required for anti-inflammatory efficacy. |
| In vivo | Nabumetone undergoes extensive first-pass metabolism to form its main active metabolite (6-MNA) in the systemic circulation, which is capable of inhibiting COX-2. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (240.92 mM)
Ethanol : 24 mg/mL (105.1 mM)
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| Keywords | Cyclooxygenase | Inhibitor | COX | inhibit | BRL 14777 | BRL-14777 | Nabumetone |
| Inhibitors Related | Ibuprofen | Acetaminophen | Paradol | Melatonin |
| Related Compound Libraries | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
