LUMIRACOXIB
- Product Name
- LUMIRACOXIB
- CAS No.
- 220991-20-8
- Chemical Name
- LUMIRACOXIB
- Synonyms
- Prexige;COX 189;CGS 35189;Lumaricoxib;LUMIRACOXIB;Unii-V91T9204hu;Prexige, Lumiracoxib;Xanthine Impurity 30;LuMiracoxib (COX-189);Lumiracoxib (CGS 35189
- CBNumber
- CB21006324
- Molecular Formula
- C15H13ClFNO2
- Formula Weight
- 293.72
- MOL File
- 220991-20-8.mol
LUMIRACOXIB Property
- 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
- form
- solid
- pka
- 4.18±0.10(Predicted)
- color
- White to light yellow
- CAS DataBase Reference
- 220991-20-8
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML2928
- Product name
- Lumiracoxib
- Purity
- ≥98% (HPLC)
- Packaging
- 10MG
- Price
- $46.6
- Updated
- 2024/03/01
- Product number
- SML2928
- Product name
- Lumiracoxib
- Purity
- ≥98% (HPLC)
- Packaging
- 50MG
- Price
- $191
- Updated
- 2024/03/01
- Product number
- 27645
- Product name
- Lumiracoxib
- Packaging
- 10mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 27645
- Product name
- Lumiracoxib
- Packaging
- 50mg
- Price
- $86
- Updated
- 2024/03/01
- Product number
- 27645
- Product name
- Lumiracoxib
- Packaging
- 100mg
- Price
- $153
- Updated
- 2024/03/01
LUMIRACOXIB Chemical Properties,Usage,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
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.
LUMIRACOXIB Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from LUMIRACOXIB manufacturers
- Product
- LUMIRACOXIB 220991-20-8
- Price
- US $9.90/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 10 mt
- Release date
- 2024-11-29
- Product
- LUMIRACOXIB 220991-20-8
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 50000KG/month
- Release date
- 2023-08-28
- Product
- LUMIRACOXIB 220991-20-8
- Price
- US $30.00/Kg/Bag
- Min. Order
- 1Kg/Bag
- Purity
- 99
- Supply Ability
- 999
- Release date
- 2020-11-09