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Lumiracoxib

Lumiracoxib (Prexige) 是强选择性有口服活性的 COX-2抑制剂，Ki 值为 0.06 μM。它是非选择性非甾体抗炎试剂，具有抗炎和解热活性，可用于骨关节炎和骨癌研究。

CAS号

220991-20-8

分子式

C15H13ClFNO2

主要靶点

COX

仅限科研使用

Cat No : CM03551

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Synonyms

COX-189|Prexige|罗美昔布

验证数据展示

  • CAS No.: 220991-20-8

    Lumiracoxib
    CAS#: 220991-20-8

产品信息

Lumiracoxib 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.

CAS号 220991-20-8
分子式 C15H13ClFNO2
主要靶点 COX
主要通路 免疫与炎症|神经科学
分子量 293.72
纯度 99.25%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 COX-189|Prexige|罗美昔布

靶点活性

COX-2(Cell-free assay):Ki:60 nM|COX-1(Cell-free assay):Ki:3 μM

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.

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).

溶解度

H2O:<1 mg/mL,Ethanol:<1 mg/mL,DMSO:55 mg/mL (187.3 mM)

动物实验

Animal Models: Female Lewis ratsFormulation: Sterile phosphate-buffered salineDosages: 0.2–2 mg/kgAdministration: Oral gavage

参考文献

1.Esser R, et al. Br J Pharmacol, 2005, 144(4), 538-550.
2.Jiao W, Zhao X, Wu G, et al. Bioactivation of Lumiracoxib in Human Liver Microsomes: Formation of GSH‐and Amino Adducts Through Acyl Glucuronide[J]. Drug Testing and Analysis. 2020, 12(6): 827-835.
3.Sun J, Zhang L, Zhang L, et al. A validated UHPLC-MS/MS method for simultaneous determination of lumiracoxib and its hydroxylation and acyl glucuronidation metabolites in rat plasma: application to a pharmacokinetic study[J]. Journal of Pharmaceutical and Biomedical Analysis. 2021: 114105.

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