Etoricoxib D4

作者: 莫小枫 | 来源:发表于2017-12-01 13:55 被阅读0次

"目录号: HY-15321S

Immunology/Inflammation-

Etoricoxib D4是Etoricoxib(MK-0663)氘代标记化合物,Etoricoxib的生物活性可参考HY-15321。

COX

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Celecoxib-Indomethacin-Acetaminophen-Paradol-Aspirin-Ibuprofen-NS-398-Rofecoxib-Diclofenac Sodium-Iguratimod-Parecoxib-Sulindac-Etoricoxib-Naproxen-Valdecoxib-

生物活性

Description

Etoricoxib D4 is a deuterium labeled Etoricoxib, which selectively inhibit COX-2 in human whole blood assays in vitro, with an IC50 value of 1.1 ± 0.1 μM for COX-2 (LPS-induced prostaglandin E2 synthesis), compared with an IC50 value of 116 ± 8 μM for COX-1 (serum thromboxane B2 generation after clotting of the blood). IC50 value: 1.1 uM (LPS-induced prostaglandin E2 synthesis)Target: COX-2In summary, Etoricoxib represents a novel agent that selectively inhibits COX-2 with 106-fold selectivity in human whole blood assays in vitro and with the lowest potency of inhibition of COX-1 compared with other reported selective agents. Single preoperative oral dose (120 mg) of Etoricoxib, given one hour before surgery, has significantly reduced the post operative pain at rest and movement and improved sleep in patients undergoing single level diskectomy without any side effects and with good patient satisfaction.

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