Lumiracoxib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lumiracoxib 是一种新型选择性 COX-2 抑制剂，IC50 和 Ki 分别为 0.14 μM 和 0.06 μM，选择性是 COX-1 的 515 倍。第四阶段。

Lumiracoxib, also known as CGS 35189 and COX 189, is a COX-2 selective inhibitor non-steroidal anti-inflammatory drug, manufactured by Novartis and still sold in few countries, including Mexico, Ecuador and the Dominican Republic, under the trade name Prexige. Since its original approval, lumiracoxib has been withdrawn from the market in several countries, mostly due to its potential for causing liver failure (sometimes requiring liver transplantation). It has never been approved for use in the United States.(In Vitro):Lumiracoxib inhibits purified COX-1 and COX-2 with Ki 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.

Lumiracoxib inhibits purified COX-1 and COX-2 with?Ki 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.

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. Animal Model:Rat model of bone cancer pain with injection of MRMT-1 tumour cells into one tibia?Dosage:10 and 30 mg/kg Administration:Oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection Result:Had an effect on mechanical hyperalgesia in a model of bone cancer pain.

CGS-35189 | CGS35189 | COX 189 | Lumiracoxib

Others

Other Targets

COX-1| COX-2

Others-Field

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220991-20-8

293.72

C15H13ClFNO2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (425.58 mM)

Clc2cccc(F)c2Nc1ccc(C)cc1CC(=O)O

2-(2-((2-chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid

(-20℃)

With Ice Pack

≥ 2 years