| 名称 | Hispidol |
| 描述 | Hispidol ((Z)-Hispidol) ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 μM. |
| 动物实验 | Hispidol is prepapred in corn oil.Rat: To study the effect of the drugs, hispidol (10 or 30 mg/Kg/day in corn oil) is administered orally once in a day, until 5 days after TNBS administration. The doses of 10 or 30 mg/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 (300 mg/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 (5-7 cm proximal to rectum) are cut and used to measure the amount of myeloperoxidase and for the histological examinations[1]. |
| 体外活性 | Hispidol demonstrates potent inhibitory effects on TNF-α-induced adhesion of monocytes to colonic epithelial cells and LPS-induced TNF-α expression, making it a promising candidate for inflammatory bowel disease (IBD) drug development. This compound not only inhibits TNF-α expression effectively (>70%)—a critical event in IBD progression—but also suppresses AP-1 transcriptional activity, which is essential for high levels of TNF-α expression. |
| 体内活性 | Oral administration of hispidol suppresses TNBS-induced colitis in a dose-dependent manner. Body weight loss and colon tissue edematous inflammation are recovered significantly. The oral administration of hispidol suppresses significantly and dose-dependently TNBS-induced rat colitis. A higher dose (30 mg/kg) of hispidol shows a similar recovery effect to that of 300 mg/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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 6.25 mg/mL (24.58 mM), Sonication is recommended.
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| 关键字 | inhibit | Hispidol | TNF Receptor | Tumor Necrosis Factor Receptor | TNFR | Inhibitor |
| 相关产品 | Cepharanthine | Acetylcysteine | Acefylline | Glucosamine | Thalidomide | Taurochenodeoxycholic Acid | Apremilast | Pomalidomide | Bergenin | Lenalidomide | Fisetin | Linalool |
| 相关库 | 细胞凋亡化合物库 | 经典已知活性库 | 血管生成库 | 抑制剂库 | NO PAINS 化合物库 | 抗心血管疾病化合物库 | 肿瘤免疫治疗小分子化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 人代谢物化合物库 |
United States
