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Lumiracoxib

Catalog No. T6574 CAS 220991-20-8

Synonyms: Prexige, COX-189

Lumiracoxib (Prexige) is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

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Lumiracoxib, CAS 220991-20-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 37.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 72.00
50 mg	In stock	$ 97.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.25%

Purity: 96.64%

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Storage & Solubility Information

Description	Lumiracoxib (Prexige) is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.
Targets&IC50	COX-2 (cell-free assay):Ki:60 nM, COX-1 (cell-free assay):Ki:3 μM
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.
Animal Research	Animal Models: Female Lewis ratsFormulation: Sterile phosphate-buffered salineDosages: 0.2–2 mg/kgAdministration: Oral gavage

Synonyms	Prexige, COX-189
Molecular Weight	293.72
Formula	C15H13ClFNO2
CAS No.	220991-20-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 55 mg/mL (187.3 mM)

References and Literature

1. Esser R, et al. Br J Pharmacol, 2005, 144(4), 538-550. 2. Jiao W, Zhao X, Wu G, et al. Bioactivation of Lumiracoxib in Human Liver Microsomes: Formation of GSH‐and Amino Adducts Through Acyl Glucuronide[J]. Drug Testing and Analysis. 2020, 12(6): 827-835. 3. Sun J, Zhang L, Zhang L, et al. A validated UHPLC-MS/MS method for simultaneous determination of lumiracoxib and its hydroxylation and acyl glucuronidation metabolites in rat plasma: application to a pharmacokinetic study[J]. Journal of Pharmaceutical and Biomedical Analysis. 2021: 114105.

Citations

1. Sun J, Zhang L, Zhang L, et al. A validated UHPLC–MS/MS method for simultaneous determination of lumiracoxib and its hydroxylation and acyl glucuronidation metabolites in rat plasma: Application to a pharmacokinetic study. Journal of Pharmaceutical and Biomedical Analysis. 2021, 201: 114105. 2. Sun J, Zhang L, Zhang L, et al. A validated UHPLC-MS/MS method for simultaneous determination of lumiracoxib and its hydroxylation and acyl glucuronidation metabolites in rat plasma: application to a pharmacokinetic study. Journal of Pharmaceutical and Biomedical Analysis. 2021: 114105. 3. Jiao W, Zhao X, Wu G, et al. Bioactivation of Lumiracoxib in Human Liver Microsomes: Formation of GSH‐and Amino Adducts Through Acyl Glucuronide. Drug Testing and Analysis. 2020, 12(6): 827-835.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Compound Library Neuronal Signaling Compound Library Orally Active Compound Library

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Keywords

Lumiracoxib 220991-20-8 Immunology/Inflammation Neuroscience COX Prexige Cyclooxygenase Inhibitor bone cancer osteoarthritis COX 189 inflammatory COX189 inhibit hyperalgesic COX-189 Metabolic Syndrome inhibitor

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