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SC-560 是一种选择性 COX-1抑制剂,IC50值为 9 nM。


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SC-560 是一种选择性 COX-1抑制剂,IC50值为 9 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 2 mg | ¥ 283 | In stock | |
| 5 mg | ¥ 453 | In stock | |
| 10 mg | ¥ 861 | In stock | |
| 25 mg | ¥ 1,930 | In stock | |
| 50 mg | ¥ 2,890 | In stock | |
| 100 mg | ¥ 4,280 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 547 | In stock |
SC-560 相关产品
| 产品描述 | SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors. |
| 靶点活性 | COX-1:9 nM., COX-2:6.3 μM |
| 体外活性 | 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。 |
| 体内活性 | 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。 |
| 激酶实验 | 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. |
| 细胞实验 | 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. |
| 动物实验 | 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. |
| 别名 | SC560 |
| 分子量 | 352.74 |
| 分子式 | C17H12ClF3N2O |
| CAS No. | 188817-13-2 |
| Smiles | COc1ccc(cc1)-n1nc(cc1-c1ccc(Cl)cc1)C(F)(F)F |
| 密度 | 1.33g/cm3 |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 35.3 mg/mL (100.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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