SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors.

COX-1:9 nM.

将COX-1与SC-560预先孵育可浓度依赖性地抑制花生四烯酸向PGE2的转化。SC-560对COX-2的IC50为6.3μM，约为对COX-1的1000倍。SC-560展示了剂量和时间依赖性地抑制HCC细胞生长的效应。同时，SC-560在剂量依赖的方式下抑制软琼脂中的集落形成，并诱导HCC细胞发生凋亡。此外，SC-560降低了抗凋亡蛋白survivin和XIAP的水平，并在剂量和时间依赖的方式中激活caspase 3和7。

在检测前 1 小时口服 10 或 30 mg/kg SC-560 可完全抑制离子刺激物刺激的 TxB2 生成，这表明 SC-560 具有口服生物利用度，可在体内抑制 COX-1。SC-560 广泛分布于大鼠组织中，CL 值接近肝血浆流量。口服后，该化合物的生物利用度低于 15%，并显示出肾毒性。

Test compound is incubated with human whole blood stimulated with bacterial LPS for 4 h, followed by capture of MPO on immobilized anti-MPO antibody coated plates. The captured MPO is washed and residual MPO activity is determined using Amplex Red and H2O2.

SC-560 is dissolved in DMSO[2].HuH-6 and HA22T/VGH cells (5000/well) are treated with various concentrations of SC-560 (5, 10, 25, 50, 100, 200 μM) and cultured for 72 h. At the end of treatment, cell viability is assessed by MTS assay.

Rat: The pharmacokinetics of SC-560 is studied in Sprague-Dawley rats after a single intravenous (i.v.) and oral dose (10 mg/kg) in polyethylene glycol (PEG) 600 and a single oral dose (10 mg/kg) in 1% methylcellulose (MC). Serial blood samples are collected via a catheter inserted in the right jugular vein and serum samples are analysed for SC-560 using reverse phase HPLC. After oral administration of SC-560 in PEG, urine is also collected for 24 h and analyzed for urinary sodium, chloride, and potassium as well as NAG.