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BI 653048 phosphate

Catalog No. T10535LCas No. 1198784-97-2

BI 653048 phosphate is a selective, orally active agonist of nonsteroidal glucocorticoid (GC) with an IC50 of 55 nM.

BI 653048 phosphate

BI 653048 phosphate

Catalog No. T10535LCas No. 1198784-97-2
BI 653048 phosphate is a selective, orally active agonist of nonsteroidal glucocorticoid (GC) with an IC50 of 55 nM.
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Product Introduction

Bioactivity
Description
BI 653048 phosphate is a selective, orally active agonist of nonsteroidal glucocorticoid (GC) with an IC50 of 55 nM.
Targets&IC50
CYP2C9:12 μM, CYP1A2:50 μM, CYP2D6:41 μM, CYP3A4:8 μM, CYP2C19:9 μM
In vitro
BI 653048 phosphate demonstrates improved drug-like properties, inhibiting CYP1A2, CYP2D6, CYP2C9, CYP2C19, and CYP3A4 with IC50 values of 50 μM, 41 μM, 12 μM, 9 μM, and 8 μM, respectively[2]. It also inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM[2] and reduces affinity for the hERG ion channel, exhibiting an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel[2].
In vivo
BI 653048 phosphate (oral administration; 3, 10, and 30 mg/kg) at 3 mg/kg shows nonsignificant decreases in ankle inflammation, pannus formation, cartilage damage, and bone resorption. At 10 mg/kg, it significantly decreases pannus formation and bone resorption (33%) and summed scores (27%). At 30 mg/kg, all parameters significantly decrease (87–96%). The ED50 value for the summed scores is 14 mg/kg [2].
Chemical Properties
Molecular Weight613.52
FormulaC23H28F4N3O8PS
Cas No.1198784-97-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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