Catalog No.S2903 Synonyms: COX-189
Molecular Weight(MW): 293.72
Lumiracoxib is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM.
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Blood concentration-time profiles for lumiracoxib following single oral administration at 10 mg/kg to (a) Hu-FRGTM mice (n = 3) and (b) to Mu-FRGTM mice (n = 3). Symbols represent concentration-time profiles from individual animals.
Biochem Pharmacol, 2017, 135:139-150. Lumiracoxib purchased from Selleck.
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|Description||Lumiracoxib is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM.|
Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm (HEK 293 cells transfected with human COX-1). In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1 (COX-1/COX-2 selectivity ratio 515). 
|In vivo||Lumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib is rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. Efficacy of Lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis is dose-dependent and similar to diclofenac. However, consistent with its low COX-1 inhibitory activity, Lumiracoxib at a dose of 100 mg/kg orally causes no ulcers and is significantly less ulcerogenic than diclofenac. |
|In vitro||DMSO||59 mg/mL (200.87 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01481610||Terminated||Kidney Failure Chronic|Arthralgia||Hospital Central Sur de Pemex||January 2012||Phase 2|
|NCT00419796||Completed||Osteoarthritis With Controlled Hypertension||Novartis||November 2006||Phase 4|
|NCT00333567||Completed||Pain||Novartis||August 2006||Phase 4|
|NCT00350155||Completed||Healthy Volunteers||Novartis||May 2006||Phase 4|
|NCT00348491||Completed||Pain||Novartis Pharmaceuticals|Novartis||February 2006||Phase 4|
|NCT00267176||Completed||Osteoarthritis|Controlled Hypertension||Novartis Pharmaceuticals|Novartis||November 2005||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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