158205-05-1
158205-05-1 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15687 英文別名
L-745337Thioflosulide
Methanesulfonamide, N-[6-[(2,4-difluorophenyl)thio]-2,3-dihydro-1-oxo-1H-inden-5-yl]-
物理化學(xué)性質(zhì)
沸點495.8±55.0 °C(Predicted)
密度1.52±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)6?+-.0.20(Predicted)
常見問題列表
生物活性
Thioflosulide (L-745337) 是一種選擇性的 COX2 抑制劑，IC50 值為 2.3 nM，具有抗炎功效。靶點
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COX-2 2.3 nM (IC 50 ) |
體內(nèi)研究
In a rat model of postoperative pain, Thioflosulide (L-745337) (40-80 μg, intrathecal) coadministered with intrathecal morphine (0.5 nmol) increases the withdrawal thresholds in a dose-dependent manner. Adding 80 μg Thioflosulide (L-745337) to 1 nmol morphine produces an antiallodynic effect greater than that of morphine at twice the dose. Thioflosulide (L-745337) (0-30 mg/kg, s.c.) combined with intrathecal morphine results in the same antiallodynic response as morphine alone. Thioflosulide (L-745337) shows anti-inflammatory activity, with the effective-dose of 0.4 mg/kg, and the maximal anti-inflammation dose of 5 mg/kg in arthritic rats.