Home Neuronal Signaling COX inhibitor Lumiracoxib For research use only.

Lumiracoxib

Synonyms: COX-189

Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM.

Lumiracoxib Chemical Structure

Lumiracoxib Chemical Structure

CAS No. 220991-20-8

Purity & Quality Control

Lumiracoxib Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

Biological Activity

Description Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM.
Targets
COX-2 [1]
(Cell-free assay)		 COX-1 [1]
(Cell-free assay)
60 nM(Ki) 3 μM(Ki)
In vitro
In vitro 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). [1]
In Vivo
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. [1]
Animal Research Animal Models Female Lewis rats
Dosages 0.2–2 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT00170872 Completed
Osteoarthritis|Rheumatoid Arthritis
Novartis
 November 2004 Phase 3
NCT00145301 Completed
Osteoarthritis
Novartis
 September 2004 Phase 3
NCT00475800 Completed
Osteoarthritis
Novartis
 January 2004 Phase 3

Chemical Information & Solubility

Molecular Weight 293.72 Formula

C15H13ClFNO2
CAS No. 220991-20-8 SDF Download Lumiracoxib SDF
Smiles CC1=CC(=C(C=C1)NC2=C(C=CC=C2Cl)F)CC(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (200.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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