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BI 653048 is a selective, orally active nonsteroidal glucocorticoid agonist (IC50: 55 nM) and an HCV NS3 protease inhibitor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $2,720 | 3-6 months | 3-6 months | |
| 50 mg | $3,580 | 3-6 months | 3-6 months | |
| 100 mg | $4,900 | 3-6 months | 3-6 months |
| 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, CYP2D6:41 μM, CYP1A2:50 μM, CYP2C19:9 μM, CYP3A4:8 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]. |
| Molecular Weight | 515.52 |
| Formula | C23H25F4N3O4S |
| Cas No. | 1198784-72-3 |
| Smiles | C([C@](CC(C)(C)C1=C(C(N)=O)C=C(F)C=C1)(C(F)(F)F)O)C2=CC=3C(N2)=CN=C(S(CC)(=O)=O)C3 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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