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SC-560

CAS号

188817-13-2

分子式

C17H12ClF3N2O

主要靶点

COX

仅限科研使用

Cat No : CM03564

Print datasheet

Synonyms

inhibit|COX-2|COX-1|COX|Cyclooxygenase|SC560|SC-560|SC 560|Inhibitor

验证数据展示

  • CAS No.: 188817-13-2

    SC-560
    CAS#: 188817-13-2

产品信息

CAS号 188817-13-2
分子式 C17H12ClF3N2O
主要靶点 COX
主要通路 神经科学|免疫与炎症
分子量 352.74
纯度 99.39%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|COX-2|COX-1|COX|Cyclooxygenase|SC560|SC-560|SC 560|Inhibitor

靶点活性

COX-1:9 nM.

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。

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。

溶解度

DMSO:35.3 mg/mL (100 mM)

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.

参考文献

1.Smith CJ, et al. Pharmacological analysis of cyclooxygenase-1 in inflammation. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13313-8.
2.Lampiasi N, et al. The selective cyclooxygenase-1 inhibitor SC-560 suppresses cell proliferation and induces apoptosis in human hepatocellular carcinoma cells. Int J Mol Med. 2006 Feb;17(2):245-52
3.Teng XW, et al. Formulation dependent pharmacokinetics, bioavailability and renal toxicity of a selective cyclooxygenase-1 inhibitor SC-560 in the rat. J Pharm Pharm Sci. 2003 May-Aug;6(2):205-10.

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