BI 653048 phosphate 

BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value 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 HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus^[3].

BI 653048 phosphate exhibits an improved drug-like properties, inhibits CP1A2 ,CYP2D6 ,CYP2C9, CYP2C19 and CYP3A4 with IC₅₀ values 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 IC₅₀ value of 100 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 ED₅₀ value for the summed scores is 14 mg/kg^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

613.52

C₂₃H₂₈F₄N₃O₈PS

1198784-97-2

O=C(N)C1=CC(F)=CC=C1C(C)(C)C[C@@](O)(CC(N2)=CC3=C2C=NC(S(=O)(CC)=O)=C3)C(F)(F)F.O=P(O)(O)O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Reeves JT, et al. Development of a large scale asymmetric synthesis of the glucocorticoid agonist BI 653048 BS H3PO4.J Org Chem. 2013 Apr 19;78(8):3616-35.  [Content Brief]

  [2]. Harcken C, et al. Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.ACS Med Chem Lett. 2014 Nov 20;5(12):1318-23.  [Content Brief]

  [3]. Montse Llinas-Brunet, et al. Latest bibliographic data on file with the International Bureau