BI 653048

BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC 50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel ( IC 50 >30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus . In Vitro BI 653048 exhibits an improved drug-like properties, inhibits CP1A2 ,CYP2D6 ,CYP2C9, CYP2C19 and CYP3A4 with IC 50 values of 50 µM, 41 µM, 12 µM, 9 µM,and 8 µM, respectively. BI 653048 reduces affinity for the hERG ion channel with an IC 50 >30 μM in recombinant HEK293 cells expressing the human ERG potassium channel. BI 653048 inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC 50 value of 100 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo BI 653048 (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 ED 50 value for the summed scores is 14 mg/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MiceDosage: 3, 10, and 30 mg/kg Administration: Oral administration Result: Exhibits significant decreases for all measured histology parameters at high doses.

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