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SC-560

SC-560

产品编号 T4101   CAS 188817-13-2
别名: SC560

SC-560 是一种选择性 COX-1抑制剂,IC50值为 9 nM。

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SC-560 Chemical Structure
SC-560, CAS 188817-13-2
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
重组蛋白限时优惠
产品目录号及名称: SC-560 (T4101)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 35.3 mg/mL(100 mM)

溶液配制表

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

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TargetMol Library Books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.
COX-2-IN-1 Flavidin Moracin T Ginsenoside Rb3 Nepafenac Dexketoprofen trometamol Thioflosulide α-​Chaconine

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 高选择性抑制剂库 经典已知活性库 NO PAINS 化合物库 含氟化合物库 细胞焦亡化合物库 线粒体靶向库 抗衰老化合物库 抗胰腺癌化合物库 抗结直肠癌化合物库

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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。

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技术支持

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。

Keywords

SC-560 188817-13-2 Immunology/Inflammation Neuroscience COX Cyclooxygenase inhibit SC 560 Inhibitor SC560 inhibitor

 

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