Lumiracoxib

Catalog No.S2903 Synonyms: COX-189

For research use only.

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

CAS No. 220991-20-8

Selleck's Lumiracoxib has been cited by 10 Publications

3 Customer Reviews

Purity & Quality Control

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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

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 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]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Female Lewis rats
  • Dosages: 0.2–2 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 59 mg/mL
(200.87 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 293.72
Formula

C15H13ClFNO2

CAS No. 220991-20-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C=C1)NC2=C(C=CC=C2Cl)F)CC(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00350155 Completed Drug: Lumiracoxib Healthy Volunteers Novartis May 2006 Phase 4
NCT00348491 Completed Drug: Lumiracoxib Pain Novartis Pharmaceuticals|Novartis February 2006 Phase 4
NCT00267176 Completed Drug: lumiracoxib Osteoarthritis|Controlled Hypertension Novartis Pharmaceuticals|Novartis November 2005 Phase 4
NCT00170872 Completed Drug: Lumiracoxib Osteoarthritis|Rheumatoid Arthritis Novartis November 2004 Phase 3
NCT00145301 Completed Drug: Lumiracoxib Osteoarthritis Novartis September 2004 Phase 3
NCT00475800 Completed Drug: Lumiracoxib Osteoarthritis Novartis January 2004 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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