Hispidol 文献数量:1 ≥98%
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| 包装规格: | 1mg 5mg 10mg 25mg 50mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(≥ 100 mg/mL) |
| 产品描述: | 基本信息 产品编号:H10343 产品名称:Hispidol CAS: 5786-54-9 储存条件 粉末 -20℃ 四年 分子式: C15H10O4 溶于液体 -80℃ 六个月 分子量 254.24 -20℃ 一个月 化学名: Solubility (25°C) 体外 DMSO ' mg/mL 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。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 3.9333mL 19.6665mL 39.3329mL 5mM 0.7867mL 3.9333mL 7.8666mL 10mM 0.3933mL 1.9666mL 3.9333mL 生物活性 产品描述 具有研究炎症性肠病的潜力,能够抑制 TNF-α 诱导的单核细胞对结肠上皮细胞的粘附,IC50 值为 0.50μM。 靶点/IC50 TNF Receptor 体外研究 Hispidol shows potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to inflammatory bowel disease (IBD).Hispidol shows strong inhibitory activities against TNF-α-induced monocytic-colonic epithelial cell adhesion as well as LPS-induced TNF-α expression, is as an excellent candidate for IBD drug development.This inhibition of TNF-α expression by hispidol corresponds to the additional inhibitory activity against AP-1 transcriptional activity, which is another transcription factor required for high level TNF-α expression. 体内研究 The oral administration of hispidol suppresses significantly and dose-dependently TNBS-induced rat colitis. Oral administration of hispidol suppresses TNBS-induced colitis in a dose-dependent manner. There is a significant recovery in body weight decrease and colon tissue edematous inflammation. A higher dose (30mg/kg) of hispidol shows a similar recovery effect to that of 300mg/kg sulfasalazine. In the colon tissues, TNBS induces a dramatic increase in the level of MPO,a biochemical marker of inflammation, which is suppressed significantly by hispidol in a dose-dependent manner. 推荐实验方法(仅供参考) 动物实验: Rats: To study the effect of the drugs, hispidol (10 or 30mg/Kg/day in corn oil) is administered orally once in a day, until 5 days after TNBS administration. The doses of 10 or 30mg/kg are selected based on previous studies. The concentration of the compound inhibiting 70% and 90% (µM) cell-to-cell adhesion is selected and regarded as the in vivo test dose (mg/kg).Sulfasalazine (300mg/Kg/day) is administered in corn oil as a positive control. On the 6th day, the rats are sacrificed and the severity of colitis and macroscopic ulceration are evaluated by two independent investigators who are blinded to the experiments. The colon tissues (5-7cm proximal to rectum) are cut and used to measure the amount of myeloperoxidase and for the histological examinations. |
| 保存条件: | -20℃ |
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