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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.
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | Backorder |
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Product Introduction
Bioactivity
Chemical Properties
| 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, CYP2C19:9 μM, CYP3A4:8 μM, CYP1A2:50 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 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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