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Lumiracoxib COX inhibitor

Name: Lumiracoxib
SKU: S2903
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S2903

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

Chemical Structure

Molecular Weight: 293.72

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.91%

99.91

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Chemical Information, Storage & Stability

Molecular Weight	293.72	Formula	C₁₅H₁₃ClFNO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	220991-20-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	COX-189			Smiles	CC1=CC(=C(C=C1)NC2=C(C=CC=C2Cl)F)CC(=O)O

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (200.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.950mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 59 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.295mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	COX-2 ^[1] (Cell-free assay) 60 nM(Ki) COX-1 ^[1] (Cell-free assay) 3 μM(Ki)
In vitro	Lumumiracoxib 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 this compound 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. This compound is rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. Efficacy of this chemical 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, it at a dose of 100 mg/kg orally causes no ulcers and is significantly less ulcerogenic than diclofenac. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15655513/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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