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BI 653048

BI 653048
BI 653048 is a selective, orally active nonsteroidal glucocorticoid agonist (IC50: 55 nM) and an HCV NS3 protease inhibitor.
Catalog No. T10535Cas No. 1198784-72-3

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BI 653048

Catalog No. T10535Cas No. 1198784-72-3

BI 653048 is a selective, orally active nonsteroidal glucocorticoid agonist (IC50: 55 nM) and an HCV NS3 protease inhibitor.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
BI 653048 is a selective, orally active nonsteroidal glucocorticoid agonist (IC50: 55 nM) and an HCV NS3 protease inhibitor.
Targets&IC50
CYP2C9:12 μM, CYP1A2:50 μM, CYP3A4:8 μM, CYP2D6:41 μM, CYP2C19:9 μM
In vitro
BI 653048 exhibits improved drug-like properties, inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19, and CYP3A4 (IC50s: 50 μM, 41 μM, 12 μM, 9 μM, and 8 μM). BI 653048 reduces affinity for the hERG ion channel with an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel. BI 653048 inhibits TNF-stimulated IL-6 production in mouse RAW cells (IC50: 100 nM) [2].
In vivo
BI 653048 (p.o.; 3, 10, and 30 mg/kg) at 3 mg/kg has nonsignificant decreases for all measured histology parameters (ankle inflammation, cartilage damage, pannus formation, 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].
Chemical Properties
Molecular Weight515.52
FormulaC23H25F4N3O4S
Cas No.1198784-72-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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