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Purity: ≥98%
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.
| ln Vitro |
Nabumetone is a highly powerful and selective COX-2 inhibitor. Nabumetone (50 μmol-2 mmol) decreases proliferation of K-562 and Meg-01 cells in a dose-dependent manner, but has no apparent apoptotic impact. Nabumetone enhances the apoptotic impact of ADR in the K-562 cell line. Furthermore, Nabumetone lowers Bcl-2 expression[1].
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| ln Vivo |
In rats, napumetone (79 mg/kg, po) reduces PGE2 exudate from the paws and paw oedema. In rats, napumetone only inhibits the generation of 6-keto-PGF1α from the gastric mucosa by 57% and does not cause any harm to the stomach[2]. In rats, napumetine (25, 50, and 100 mg/kg, i.p.) enhances mucus secretion generated by stress and dose-dependently prevents the rise in DDC-induced mucus secretion. Rats' stress-induced ulcer index is dramatically suppressed by napumetone (25 mg/kg, ip)[3].
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| References |
[1]. Vural F, et al. Cyclo-oxygenase 2 inhibitor, nabumetone, inhibits proliferation in chronic myeloid leukemia cell lines. Leuk Lymphoma. 2005 May;46(5):753-6.
[2]. Melarange R, et al. 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 |
| Molecular Formula |
C15H16O2
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| Molecular Weight |
228.29
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| CAS # |
42924-53-8
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| Related CAS # |
Nabumetone-d3;1216770-08-9
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| SMILES |
O(C([H])([H])[H])C1C([H])=C([H])C2C([H])=C(C([H])=C([H])C=2C=1[H])C([H])([H])C([H])([H])C(C([H])([H])[H])=O
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| InChi Key |
BLXXJMDCKKHMKV-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-(6-methoxynaphthalen-2-yl)butan-2-one
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3804 mL | 21.9020 mL | 43.8039 mL | |
| 5 mM | 0.8761 mL | 4.3804 mL | 8.7608 mL | |
| 10 mM | 0.4380 mL | 2.1902 mL | 4.3804 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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