| CAS NO: | 42924-53-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| 25g | 电议 |
| 50g | 电议 |
| 100g | 电议 |
| Molecular Weight (MW) | 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) | |
| Other info | 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 |
| Synonyms | BRL-14777; Nabumetone, Relafen, BRL14777; BRL 14777; Relifex, Gambaran, Arthraxan |
| 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. 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. |
|---|---|
| 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 | Rats and guinea pigs |
| Formulation & Dosage | N/A |
| References | Drugs. 2004;64(20):2315-43; discussion 2344-5; J Pharm Pharmacol. 1982 Sep;34(9):562-9. |
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