| CAS: | 220991-20-8 |
| MF: | C15H13ClFNO2 |
| MW: | 293.72 |
| EINECS: | 1308068-626-2 |
| Product Categories: | Inhibitors;PREXIGE;Aromatics Compounds;Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol File: | 220991-20-8.mol |
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| LUMIRACOXIB Chemical Properties |
| Melting point | 139-141°C |
| Boiling point | 395.7±42.0 °C(Predicted) |
| density | 1.363±0.06 g/cm3(Predicted) |
| storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| solubility | ≥29.4 mg/mL in DMSO; insoluble in H2O; ≥27.15 mg/mL in EtOH with ultrasonic |
| pka | 4.18±0.10(Predicted) |
| form | solid |
| CAS DataBase Reference | 220991-20-8 |
| LUMIRACOXIB Usage And Synthesis |
| Description | As a second-generation, selective cyclooxygenase (COX-2) inhibitor, lumiracoxib is devoid of the gastrointestinal issues that plague other non-selective, nonsteroidal, anti-inflammatory drugs (NSAIDs) that crossover to COX-1. As an inhibitor of the inducible COX-2 that is up-regulated in pathological processes of pain and inflammation, lumiracoxib blocks the conversion of arachidonic acid to prostaglandins, the mediators of the pathological effects. It’s mode of binding to COX-2 has been found to differ from the other selective COX-2 inhibitors; the carboxylic acid forms hydrogen bonds with Tyr-385 and Ser-530 in the catalytic site rather than seeking interactions within the larger hydrophobic side pocket. Since lumiracoxib is mainly metabolized by CYP2C9, a study evaluating the co-administration of lumiracoxib with fluconazole, a potent inhibitor of CYP2C9, was conducted, and it concluded that there was no need for lumiracoxib dose adjustment, since changes in the systemic exposure were not significant. No serious adverse effects were reported, but in the small number of cases where treatment was discontinued, Gastro intestinal (GI) and musculoskeletal complaints were common. |
| Description | Lumiracoxib is a selective inhibitor of COX-2 with IC50 values of 0.13 and 67 μM for COX-2 and COX-1, respectively, in isolated human whole blood. It reduces increases in the levels of prostaglandin E2 (PGE2; ) induced by IL-1β in human dermal fibroblasts (IC50 = 0.14 μM), as well as in LPS-stimulated RAW 264.7 cells when used at concentrations ranging from 1 to 100 μM., Lumiracoxib (3 and 10 mg/kg) also decreases LPS-induced increases in the levels of PGE2 in a rat model of air pouch inflammation. It reduces M. tuberculosis-induced increases in hind paw volume and the radiological and histopathological severity of arthritic lesions in a rat model of chronic arthritis when administered at a dose of 2 mg/kg. |
| Chemical Properties | Pale Yellow Solid |
| Originator | Novartis AG (Switzerland) |
| Uses | Lumiracoxib is a selective cyclooxygenase-2-(COX-2) inhibitor and an anti-inflammatory agent (1,2,3,4). |
| Uses | Selective cyclooxygenase-2-(COX-2) inhibitor. Anti-inflammatory. |
| Uses | antiinflammatory, analgesic, antiarthritic |
| Definition | ChEBI: An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthrit s, but was withdrawn due to concersns of hepatotoxicity. |
| Brand name | Prexige |
| Biochem/physiol Actions | Lumiracoxib (COX189) is an orally active, potent and selective cyclooxygenase-2 inhibitor (Ki = 60 nM/COX-2 vs. 3.2 μM/COX-1) that inhibits COX-2-mediated PGE2 production in human whole blood (IC50 = 130 nM; stimulation = 50 μM A23187), but not COX-1-dependent TxB2 production (IC50 = 67 μM; stimulation = 10 μg/mL LPS). Lumiracoxib shows in vivo anti-inflammatory efficacy against carrageenan-induced paw oedema (ED30 = 0.35 mg/kg p.o.), CFA-induced hyperalgesia (ED30 = 5.1 mg/kg p.o.), as well as adjuvant-induced arthritis (ED50 = 3 mg/kg/day p.o.) in rats in vivo. |
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Packing &shipping&Payment
Packing:25kg/drum
Shipping:by sea or by air
Payment:T/T,western union,moneygram
Packaging Details drum
Port:Tianjin
Lead Time :
| Quantity(Kilograms) | 1 - 10000 | >10000 |
| Est. Time(days) | 5 | To be negotiated |
Company information
Hebei Mojin Biotechnology Co., Ltd, Our company is a professional in 4'-Methylacetophenone,Levamisole hydrochloride ,N-Methylformamide and other chemical reagents research and development production enterprises. Our business covers more than 30 countries, most of the big customers come from Europe, America and other countries in the world, we can guarantee the quality and price. In recent decades, with the efforts of all employees, we have established many cooperative companies in shandong, henan, guangdong and other places. Our corporate purpose is based on the market, enhance the strength, take the road of scientific and environmental sustainable development, relying on the country. Technology r & d center, increase the investment in r & d, based on the domestic market, expand the international market, manufacturing quality products, sincere service to the society, into a modern, ecological, scientific and technological enterprise world.
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