GA135780 188817-13-2
SC-560
属性
密度 1.3300
熔点 1.56
沸点 440.58° C at 760 mmHg
存贮条件 储存温度2-8°C
描述
产品介绍 Selective cyclooxygenase-1 (COX-1) inhibitor, exhibiting 700-fold selectivity for COX-1 over COX-2.
别名 5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑;5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethyl pyrazole; 5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
生化机理 SC 560 is reported to be a Cox-1 and Cox-2 inhibitor, and is highly selective for Cox-1 (IC50 of 0.009 μM) over Cox-2 (IC50 of 6.3 μM). SC 560 also inhibits UTP-stimulated and basal cAMP levels. Cox-1 is shown to catalyze the conversion of Arachidonic Acid (20:4, n-6) (sc-200770) into PGH2 (Prostaglandin H2, sc-201266), which is the precursor of thromboxanes and other prostaglandins, therefore SC 560 also suppresses TXB2 (Thromboxane B2, sc-201452) and PGE2 (Prostaglandin E2, sc-201225) production. SC 560 also displays the ability to induce cell growth inhibition by causing cell cycle arrest at the G1 phase. Mechanistic studies show that SC 560 causes apoptosis of cells by eliciting reactive oxygen species and simultaneously decreasing the levels of anti-apoptotic proteins XIAP and survivin. Additional experiments suggest that SC 560 also activates caspase-3 and caspase-7 which results in apoptosis of cells.
应用 A highly potent and selective inhibitor of Cox-1
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