[CAS NO. 220991-20-8] Lumiracoxib

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PRODUCTS SPECIFICATIONS [220991-20-8]

Catalog

SLK-S2903

Brand

Selleck

CAS

220991-20-8

DESCRIPTION [220991-20-8]

Overview

MDL	MFCD07186254
Molecular Weight	293.72
Molecular Formula	C15H13ClFNO2
SMILES	N(C1=C(CC(O)=O)C=C(C)C=C1)C2=C(Cl)C=CC=C2F

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	0.0681 mL	0.3405 mL	0.6809 mL

Description

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

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.

References

[1] Esser R, et al. Br J Pharmacol, 2005, 144(4), 538-550.

Synonyms

Benzeneacetic acid, 2-[(2-chloro-6-fluorophenyl)amino]-5-methyl-

2-[(2-Chloro-6-fluorophenyl)amino]-5-methylbenzeneacetic acid

COX 189

Lumiracoxib

Prexige

CGS 35189

2-[2-(2-Chloro-6-fluorophenylamino)-5-methylphenyl]acetic acid

[2-[(2-Chloro-6-fluorophenyl)amino]-5-methylphenyl]acetic acid