Other
CN
EU
USA
Description: Nabumetone (formerly BRL-14777; BRL14777; Relafen, Relifex, Gambaran, Arthraxan), a non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor and a prodrug with potential anti-inflammatory activity. It has an active metabolite that also inhibits COX. As a prodrug, nabumetone itself is non-acidic and undergoes first-pass metabolism extensively following absorption, to form the main circulating active metabolite (6-MNA) which is a much more potent COX-2 inhibitor.
References: Drugs. 2004;64(20):2315-43; discussion 2344-5; J Pharm Pharmacol. 1982 Sep;34(9):562-9.
Chemical Name: 4-(6-methoxynaphthalen-2-yl)butan-2-one
InChi Key: BLXXJMDCKKHMKV-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H16O2/c1-11(16)3-4-12-5-6-14-10-15(17-2)8-7-13(14)9-12/h5-10H,3-4H2,1-2H3
SMILES Code: CC(CCC1=CC=C2C=C(OC)C=CC2=C1)=O
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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.
Cell Assay: 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.
Drugs. 2004;64(20):2315-43; discussion 2344-5; J Pharm Pharmacol. 1982 Sep;34(9):562-9.
Purity ≥98%
COA
MSDS
NMR