Lumiracoxib

Catalog No.S2903 Synonyms: COX-189

Lumiracoxib Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 270 In stock
USD 170 In stock
USD 270 In stock
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2 Customer Reviews

  • 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.

    Blood concentration-time profiles for lumiracoxib following single oral administration at 10 mg/kg to male C57bl/6J mice. Symbols represent concentration-time profiles from individual animals.

    Xenobiotica, 2016, 18:1-9.. Lumiracoxib purchased from Selleck.

Purity & Quality Control

Choose Selective COX Inhibitors

Biological Activity

Description Lumiracoxib 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

Animal Research:[1]
+ Expand
  • Animal Models: Female Lewis rats
  • Formulation: Sterile phosphate-buffered saline
  • Dosages: 0.2–2 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 293.72
Formula

C15H13ClFNO2

CAS No. 220991-20-8
Storage powder
Synonyms COX-189

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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

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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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID