Lumiracoxib

Catalog No.S2903 Batch:S290301

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Technical Data

Formula

C15H13ClFNO2
Molecular Weight 293.72 CAS No. 220991-20-8
Solubility (25°C)* In vitro DMSO 59 mg/mL (200.87 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Lumiracoxib (COX-189) 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 (from reference)

Animal Study:[1]
  • Animal Models

    Female Lewis rats

  • Dosages

    0.2–2 mg/kg

  • Administration

    Oral gavage

Customer Product Validation

Data from [Data independently produced by , , Cancer Lett, 2019, 442:453-463]

Data from [Data independently produced by , , Biochem Pharmacol, 2017, 135:139-150]

Data from [Data independently produced by , , Xenobiotica, 2016, 18:1-9.]

Selleck's Lumiracoxib has been cited by 12 publications

Catalytically active phospholipase A2 myotoxin from Crotalus durissus terrificus induces proliferation and differentiation of myoblasts dependent on prostaglandins produced by both COX-1 and COX-2 pathways [ Int J Biol Macromol, 2021, 187:603-613] PubMed: 34314795
IL-1β and TNF-α Modulation of Proliferated and Committed Myoblasts: IL-6 and COX-2-Derived Prostaglandins as Key Actors in the Mechanisms Involved [ Cells, 2020, 9(9)E2005] PubMed: 32882817
Low-Dose Aspirin Treatment Attenuates Male Rat Salt-Sensitive Hypertension via Platelet Cyclooxygenase 1 and Complement Cascade Pathway. [ J Am Heart Assoc, 2020, 9(1):e013470] PubMed: 31852420
Metabolic targeting synergizes with MAPK inhibition and delays drug resistance in melanoma [Brummer C Cancer Lett, 2019, 442:453-463] PubMed: 30481565
Restricting Glycolysis Preserves T Cell Effector Functions and Augments Checkpoint Therapy. [ Cell Rep, 2019, 29(1):135-150] PubMed: 31577944
Cyclooxygenase-2 inhibition reduces anxiety-like behavior and normalizes enhanced amygdala glutamatergic transmission following chronic oral corticosterone treatment. [ Neurobiol Stress, 2019, 11:100190] PubMed: 31467944
Detection of Cyclooxygenase-2-Derived Oxygenation Products of the Endogenous Cannabinoid 2-Arachidonoylglycerol in Mouse Brain [ ACS Chem Neurosci, 2018, 9(7):1552-1559] PubMed: 29722963
The pharmacokinetics and metabolism of lumiracoxib in chimeric humanized and murinized FRG mice. [Dickie AP, et al. Biochem Pharmacol, 2017, 135:139-150] PubMed: 28351678
Lumiracoxib metabolism in male C57bl/6J mice: characterisation of novel in vivo metabolites [P Dickie A Xenobiotica, 2017, 47(6):538-546] PubMed: 27430634
Cyclooxygenase-2 inhibition reduces stress-induced affective pathology. [ Elife, 2016, 5] PubMed: 27162170

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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