1. Immunology/Inflammation
  2. COX
  3. Lumiracoxib

Lumiracoxib (Synonyms: COX-189)

Cat. No.: HY-13507
Handling Instructions

Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a Ki value of 0.06 μM. Lumiracoxib acts as a nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research.

For research use only. We do not sell to patients.

Lumiracoxib Chemical Structure

Lumiracoxib Chemical Structure

CAS No. : 220991-20-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 55 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Description

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].

IC50 & Target[1]

COX-2

0.06 μM (Ki)

COX-1

3 μM (Ki)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat model of bone cancer pain with injection of MRMT-1 tumour cells into one tibia[1] 
Dosage: 10 and 30 mg/kg
Administration: Oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection
Result: Had an effect on mechanical hyperalgesia in a model of bone cancer pain.
Molecular Weight

293.72

Formula

C₁₅H₁₃ClFNO₂

CAS No.
SMILES

O=C(O)CC1=CC(C)=CC=C1NC2=C(F)C=CC=C2Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (851.15 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4046 mL 17.0230 mL 34.0460 mL
5 mM 0.6809 mL 3.4046 mL 6.8092 mL
10 mM 0.3405 mL 1.7023 mL 3.4046 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (7.08 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LumiracoxibCOX-189COX189COX 189COXCyclooxygenaseOAhyperalgesicinflammatorybone cancerMetabolic SyndromeosteoarthritisInhibitorinhibitorinhibit

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