LUMIRACOXIB
- CAS No.
- 220991-20-8
- Chemical Name:
- LUMIRACOXIB
- Synonyms
- Prexige;COX 189;CGS 35189;Lumaricoxib;Unii-V91T9204hu;Prexige, Lumiracoxib;Xanthine Impurity 30;LuMiracoxib (COX-189);Lumiracoxib (CGS 35189;Lumiracoxib, COX-189, Prexige
- CBNumber:
- CB21006324
- Molecular Formula:
- C15H13ClFNO2
- Molecular Weight:
- 293.72
- MDL Number:
- MFCD07186254
- MOL File:
- 220991-20-8.mol
- MSDS File:
- SDS
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 |
color | White to light yellow |
CAS DataBase Reference | 220991-20-8 |
EWG's Food Scores | 1 |
FDA UNII | V91T9204HU |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302 | |||||||||
Precautionary statements | P264-P270-P301+P312-P501 | |||||||||
NFPA 704 |
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LUMIRACOXIB price More Price(24)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML2928 | Lumiracoxib ≥98% (HPLC) | 220991-20-8 | 10MG | $46.6 | 2024-03-01 | Buy |
Sigma-Aldrich | SML2928 | Lumiracoxib ≥98% (HPLC) | 220991-20-8 | 50MG | $191 | 2024-03-01 | Buy |
Cayman Chemical | 27645 | Lumiracoxib | 220991-20-8 | 10mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 27645 | Lumiracoxib | 220991-20-8 | 50mg | $86 | 2024-03-01 | Buy |
Cayman Chemical | 27645 | Lumiracoxib | 220991-20-8 | 100mg | $153 | 2024-03-01 | Buy |
LUMIRACOXIB Chemical Properties,Uses,Production
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
antiinflammatory, analgesic, antiarthritic
Uses
Selective cyclooxygenase-2-(COX-2) inhibitor. Anti-inflammatory.
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.
LUMIRACOXIB Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 | sales@hbmojin.com | China | 12446 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29798 | 60 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9308 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32836 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29888 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 | alice@crovellbio.com | China | 8820 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | sales@chemdad.com | China | 39916 | 58 |
Shenzhen Excellent Biotech Co., Ltd. | 13480692018 | ramyan@ex-biotech.com | CHINA | 954 | 58 |
Jurong Coupling Biotechnology Co., Ltd. | 13656108824 | coupling278191416@hotmail.com | CHINA | 184 | 58 |
View Lastest Price from LUMIRACOXIB manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2023-08-29 | LUMIRACOXIB
220991-20-8
|
US $0.00 / KG | 1KG | 99% | 50000KG/month | Hebei Mojin Biotechnology Co., Ltd | ||
2021-09-29 | LUMIRACOXIB
220991-20-8
|
US $9.90 / KG | 1KG | 99% | 10 mt | Hebei Guanlang Biotechnology Co., Ltd. | ||
2020-11-16 | LUMIRACOXIB
220991-20-8
|
US $30.00 / Kg/Bag | 1Kg/Bag | 99 | 999 | Longyan Tianhua Biological Technology Co., Ltd |
- LUMIRACOXIB
220991-20-8
- US $0.00 / KG
- 99%
- Hebei Mojin Biotechnology Co., Ltd
- LUMIRACOXIB
220991-20-8
- US $9.90 / KG
- 99%
- Hebei Guanlang Biotechnology Co., Ltd.
- LUMIRACOXIB
220991-20-8
- US $30.00 / Kg/Bag
- 99
- Longyan Tianhua Biological Technology Co., Ltd