product name Nabumetone
Description: Nabumetone (also known as BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX. Nabumetone is a nonsteroidal anti-inflammatory prodrug. Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially COX-2
References: Drugs. 2004;64(20):2315-43; discussion 2344-5; J Pharm Pharmacol. 1982 Sep;34(9):562-9.
228.29
Formula
C15H16O2
CAS No.
42924-53-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 46 mg/mL (201.5 mM)
Water: <1 mg/mL
Ethanol: 25 mg/mL (109.5 mM)
Solubility (In vivo)
Synonyms
BRL-14777
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19408916
| In Vitro |
In vitro activity: Nabumetone is a nonsteroidal anti-inflammatory prodrug. Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially COX-2. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Nabumetone displays acute anti-inflammatory activity in the carrageenan-induced oedema model in rats and the ultraviolet-induced erythema model in guinea-pigs. Its activity in these tests is greater than that of aspirin but less than that of naproxen and indomethacin. In the cotton pellet-induced granuloma model in the rat, Nabumetone is active and produces no signs of toxicity at doses much greater than the lowest effective dose, unlike aspirin, naproxen or indomethacin. Nabumetone is also active in the adjuvant-induced arthritis test in rats. In contrast to aspirin, indomethacin and naproxen, Nabumetone is well tolerated by the stomach of fasted rats at doses in excess of those with anti-inflammatory activity. |
| Animal model | |
| Formulation & Dosage | |
| References | Drugs. 2004;64(20):2315-43; discussion 2344-5; J Pharm Pharmacol. 1982 Sep;34(9):562-9. |
