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BI 653048 phosphate

Catalog No. T10535L   CAS 1198784-97-2

BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).

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BI 653048 phosphate Chemical Structure
BI 653048 phosphate, CAS 1198784-97-2
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).
Targets&IC50 CYP2C9:12 μM, CYP1A2:50 μM, CYP2D6:41 μM, CYP3A4:8 μM, CYP2C19:9 μM
In vitro 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 inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM[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].
In vivo 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].
Molecular Weight 613.52
Formula C23H28F4N3O8PS
CAS No. 1198784-97-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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

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Keywords

BI 653048 phosphate 1198784-97-2 Metabolism P450 BI 653048 Phosphate BI-653048 Phosphate BI653048 Phosphate inhibitor inhibit

 

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