Lumiracoxib罗美昔布,220991-20-8

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Lumiracoxib

CAS No. : 220991-20-8

MCE 国际站：Lumiracoxib

产品活性：Lumiracoxib 是一种强效、选择性、口服活性 COX-2 抑制剂，K_i 值为 0.06 μM。Lumiracoxib 是一种非选择性非甾体抗炎试剂 (NSAID)，具有抗炎、解热活性。Lumiracoxib 可用于骨关节炎和骨癌研究。

研究领域：Immunology/Inflammation

作用靶点：COX

In Vitro: Lumiracoxib inhibits purified COX-1 and COX-2 with K_i values of 3 μM and 0.06 μM, respectively. In cellular assays, Lumiracoxib has an IC₅₀ of 0.14 μM in COX-2-expressing dermal fibroblasts, but causesno inhibition of COX-1 at concentrations up to 30 μM in HEK293 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.

In Vivo: Lumiracoxib (oral administration; 10 and 30 mg/kg; single dose) significantly reverses the established hyperalgesia with a maximal 58% reversal observed 3 h following administration in rat model.
Lumiracoxib (oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection) significantly attenuates the weight-bearing difference observed on days 14, 17 and 20. The repeated administration significantly reverses static allodynia measured 90 min following the final administration.It significantly reduces the radiologically observed structural changes 20 days after inoculation of MRMT-1 cells in rat.

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