107889-32-7
107889-32-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15825 英文別名
LY 1780025-[[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]thiazolidin-4-one
4-Thiazolidinone, 5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-
物理化學(xué)性質(zhì)
沸點(diǎn)489.9±45.0 °C(Predicted)
密度1.139±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)11.15±0.50(Predicted)
常見(jiàn)問(wèn)題列表
生物活性
LY 178002 是一種有效的 5-lipoxygenase (5-LPO) ，phospholipase A2 抑制劑，對(duì) 5-lipoxygenase 的 IC50 值為 0.6 μM，能夠抑制人多形核白細(xì)胞產(chǎn)生 LTB4，同時(shí)可相對(duì)較弱地抑制 cyclooxygenase 的活性。靶點(diǎn)
|
5-LPO 0.6 μM (IC 50 ) |
PLA2 6.3 μM (IC 50 ) |
FCO 4.2 μM (IC 50 ) |
Cyclooxygenase
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體外研究
LY178002 inhibits the generation of LTB4, PLA2 and FCO with IC 50 s of 0.1, 6.3 and 4.2 μM .
體內(nèi)研究
LY 178002 (50 mg/kg) inhibits soft tissue swelling in the uninjected paw by 81%, and inhibits bone damage in rats. The minimum effective dose for LY178002 is 10 mg/kg p.o. In the established FCA model LY178002 at 50 mg/kg p.o. inhibits the uninjected paw swelling by 75%.