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| Bioactivity |
Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a Ki value of 0.06 μM[1]. Lumiracoxib acts as a nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research[1][2]. |
| Invitro |
Lumiracoxib inhibits purified COX-1 and COX-2 with Ki values of 3 μM and 0.06 μM, respectively. In cellular assays, Lumiracoxib has an IC50 of 0.14 μM in COX-2-expressing dermal fibroblasts, but causesno inhibition of COX-1 at concentrations up to 30 μM in HEK293 cells transfected with human COX-1[1].In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1[1]. |
| In Vivo |
Lumiracoxib (oral administration; 10 and 30 mg/kg; single dose) significantly reverses the established hyperalgesia with a maximal 58% reversal observed 3 h following administration in rat model[1].Lumiracoxib (oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection) significantly attenuates the weight-bearing difference observed on days 14, 17 and 20. The repeated administration significantly reverses static allodynia measured 90 min following the final administration.It significantly reduces the radiologically observed structural changes 20 days after inoculation of MRMT-1 cells in rat[1]. Animal Model: |
| Name |
Lumiracoxib |
| CAS |
220991-20-8 |
| Formula |
C15H13ClFNO2 |
| Molar Mass |
293.72 |
| Appearance |
Solid |
| Transport |
Room temperature in continental US; may vary elsewhere. |
| Storage |
| Powder |
-20°C |
3 years |
|
4°C |
2 years |
| In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
| Reference |
[1]. Ronald Esser, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50. [2]. Alyson Fox, et al. Anti-hyperalgesic activity of the cox-2 inhibitor lumiracoxib in a model of bone cancer pain in the rat. Pain |
