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SC-560  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥100mg/mL）
产品描述：基本信息 产品编号： S10892 产品名称： SC-560 CAS: 188817-13-2   储存条件 粉末 -20℃ 四年     分子式： C17H12ClF3N2O 溶于液体 -80℃ 6个月 分子量： 352.74 -20℃ 1个月 化学名：  5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole Solubility (25°C)：   体外:   DMSO 70mg/mL (198.44mM) Ethanol 70mg/mL (198.44mM) Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.8349mL 14.1747mL 28.3495mL 5mM 0.5670mL 2.8349mL 5.6699mL 10mM 0.2835mL 1.4175mL 2.8349mL 50mM 0.0567mL 0.2835mL 0.5670mL   生物活性 产品描述 一种有效，选择性的COX-1抑制剂。 靶点 COX-1 (Cell-free assay) COX-2 (Cell-free assay) 9nM 6.3μM   体外研究 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 6.3μM,nearly 1,000-fold higher than with COX-1.SC-560 shows 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. 体内研究 Oral dosing with either 10 or 30mg/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.The drug displays low less than 15% and formulation dependent bioavailability after oral administration and demonstrates kidney toxicity.   推荐实验方法(仅供参考) 细胞实验:   HuH-6 and HA22T/VGH cells (5000/well) are treated with various concentrations of SC-560 (5,10,25,50,100,200μM) and cultured for 72h.At the end of treatment,cell viability is assessed by MTS assay.   动物实验:   Rats:The pharmacokinetics of SC-560 is studied in Sprague-Dawley rats after a single intravenous (i.v.) and oral dose (10mg/kg) in polyethylene glycol (PEG) 600 and a single oral dose (10mg/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 24h and analyzed for urinary sodium,chloride,and potassium as well as NAG.
保存条件：-20℃

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