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Synonyms | COX-189 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C15H13ClFNO2 |
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分子量 | 293.72 | CAS No. | 220991-20-8 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | 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. |
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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] |
キナーゼアッセイ | Inhibition of purified COX-1 and COX-2 | |
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Purified enzyme preparations with control activities of 80 nmol of O2 consumption min−1 are pretreated with inhibitors at 37°C for various lengths of time (0–60 min). Arachidonic acid (20 μM) is then added, and O2 consumption measured using an oxygen electrode. Kinetic parameters are calculated. | ||
動物実験 | 動物モデル | Female Lewis rats |
投薬量 | 0.2–2 mg/kg | |
投与方法 | Oral gavage |
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.]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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