Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SC-560 是一种选择性 COX-1抑制剂,IC50值为 9 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 283 | 现货 | ||
5 mg | ¥ 453 | 现货 | ||
10 mg | ¥ 861 | 现货 | ||
25 mg | ¥ 1,930 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,280 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
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. |
体外活性 | Preincubation of COX-1 with SC-560 inhibits the conversion of arachidonic acid to PGE2 in a concentration-dependent manner. The IC50 of SC-560 for COX-2 is 6.3 μM, nearly 1,000-fold higher than with COX-1. SC-560 exhibits a dose and time-dependent inhibitory effect on HCC cell growth. SC-560 also inhibits colony formation in soft agar and induces apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreases the levels of the anti-apoptotic proteins survivin and XIAP and activates caspase 3 and 7 in a dose and time-dependent fashion. |
体内活性 | Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2production, indicating that SC-560 is orally bioavailable and inhibits COX-1 in vivo. SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. After oral administration, the drug exhibits low less than 15% formulation-dependent bioavailability and demonstrates kidney toxicity. |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.3 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8349 mL | 14.1747 mL | 28.3495 mL | 70.8737 mL |
5 mM | 0.567 mL | 2.8349 mL | 5.6699 mL | 14.1747 mL | |
10 mM | 0.2835 mL | 1.4175 mL | 2.8349 mL | 7.0874 mL | |
20 mM | 0.1417 mL | 0.7087 mL | 1.4175 mL | 3.5437 mL | |
50 mM | 0.0567 mL | 0.2835 mL | 0.567 mL | 1.4175 mL | |
100 mM | 0.0283 mL | 0.1417 mL | 0.2835 mL | 0.7087 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SC-560 188817-13-2 Immunology/Inflammation Neuroscience COX Cyclooxygenase inhibit SC 560 Inhibitor SC560 inhibitor