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DuP-697  

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包装规格：1mg 10mg in glass bottle
产品描述：基本信息 产品编号： D10776 产品名称： DuP-697 CAS: 88149-94-4   储存条件 粉末 -20℃ 四年     分子式： C17H12BrFO2S2 溶于液体     分子量 411.31     化学名：  5-bromo-2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)thiophene Solubility (25°C)：   体外:   DMSO   Ethanol   Water   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。   生物活性 产品描述 一种有效，不可逆，选择性和口服活性的COX-2抑制剂(对于人COX-2和COX-1，IC50分别为10nM和800nM)。DuP-697对HT29大肠癌细胞具有抗增殖作用(IC50为42.8nM)，抗血管生成和促凋亡作用。 靶点 hCOX-2 10nM(IC50) hCOX-1 800nM(IC50) 体外研究 DuP-697 (0-100nM; 24 hours; HT29 cells) treatment shows antiproliferative with an IC50 value of 42.8nM DuP-697 (25-100nM; 72 hours; HT29 cells) treatment causes concentration dependent apoptosis in HT29 cells. The percentage of UR (apoptosis portion) area increases gradually according to the concentration of DuP-697 from 7% in control group to 52% in 100nM DuP-697 DuP-697 in 100, 10 and 1nM concentrations cause antiangiogenic effect. Antiangiogenic scores of DuP-697 are 1.2, 0.8 and 0.5, respectively Cell Proliferation Assay Cell Line: HT29 cells Concentration: 0nM,12.5nM,25nM,50nM,100nM Incubation Time: 24 hours Result: Exhibited decreasing CI values in a concentration dependent manner. Showed statistically significant cytotoxic effect. Apoptosis Analysis Cell Line: HT29 cells Concentration: 25nM,50nM,100nM Incubation Time: 72 hours Result: Caused concentration dependent apoptosis in HT29 cells. 体内研究 DuP-697 is a potent inhibitor of paw swelling in nonestablished and established adjuvant arthritis in rats (ED50 = 0.03 and 0.18mg/kg/day, respectively). DuP-697 has no effect on phenylquinone writhing in rats (ED50 greater than 100mg/kg), but is analgetic against inflammation-related pain in the Randall-Selitto assay (ED50 = 3.5mg/kg) and is a very potent antipyretic agent (ED50 = 0.05mg/kg). DuP-697 (5mg/kg i.v.) does not alter renal blood flow or the renal vascular response to angiotensin II in furosemide-pretreated, volume-depleted rats DuP-697 is a moderate inhibitor of bull seminal vesicle prostaglandin (PG) synthesis (IC50 of 24μM) and a potent inhibitor of rat brain PG synthesis (IC50 of 4.5μM) but was ineffective against rat kidney PG synthesis (IC50 of 75μM)
保存条件：-20℃

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