CAS NO: | 1198784-97-2 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with anIC50value of 55 nM[1]. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM)[2]. BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCVNS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus[3]. | ||||||||
IC50& Target[2] |
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体外研究 (In Vitro) | BI 653048 phosphate exhibits an improved drug-like properties, inhibits CP1A2 ,CYP2D6 ,CYP2C9, CYP2C19 and CYP3A4 with IC50values of 50 μM, 41 μM, 12 μM, 9 μM,and 8 μM, respectively[2].BI 653048 phosphate reduces affinity for the hERG ion channel with an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel[2].BI 653048 phosphate inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50value of 100 nM[2]. | ||||||||
体内研究 (In Vivo) | BI 653048 phosphate (oral administration; 3, 10, and 30 mg/kg) at 3 mg/kg has nonsignificant decreases for all measured histology parameters (ankle inflammation, pannus formation, cartilage damage, and bone resorption), Mid-dose (10 mg/kg) treatment significantly decreases pannus and bone resorption (33%) as well as summed scores (27%), while at high dose (30 mg/kg), all parameters are significantly decreased (87–96%). The ED50value for the summed scores is 14 mg/kg[2].
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Clinical Trial | |||||||||
分子量 | 613.52 | ||||||||
Formula | C23H28F4N3O8PS | ||||||||
CAS 号 | 1198784-97-2 | ||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |