| 名称 | Lumiracoxib |
| 描述 | 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. |
| 动物实验 | Animal Models: Female Lewis ratsFormulation: Sterile phosphate-buffered salineDosages: 0.2–2 mg/kgAdministration: Oral gavage |
| 体外活性 | 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). |
| 体内活性 | 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. |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 55 mg/mL (187.3 mM)
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| 关键字 | Cyclooxygenase | Inhibitor | bone cancer | osteoarthritis | COX 189 | inflammatory | COX189 | inhibit | hyperalgesic | COX | Metabolic Syndrome | Lumiracoxib |
| 相关产品 | Ibuprofen | Acetaminophen | Salicylamide | Diclofenac sodium | Diclofenac Potassium | Paradol | Indomethacin sodium hydrate | Trometamol | Glafenine | Revaprazan hydrochloride |
| 相关库 | 高选择性抑制剂库 | 神经退行性疾病化合物库 | 经典已知活性库 | EMA 上市药物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗癌上市药物库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌药物库 |
United States
