1. BI 653048

BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.

For research use only. We do not sell to patients.

BI 653048 Chemical Structure

BI 653048 Chemical Structure

CAS No. : 1198784-72-3

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Description

BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM[1]. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM)[2]. BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus[3].

IC50 & Target

IC50: Glucocorticoid (GC)[1]

In Vitro

BI 653048 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 reduces affinity for the hERG ion channel with an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel[2].
BI 653048 inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BI 653048 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[2]
Dosage: 3, 10, and 30 mg/kg
Administration: Oral administration
Result: Exhibits significant decreases for all measured histology parameters at high doses.
Clinical Trial
Molecular Weight

515.52

Formula

C23H25F4N3O4S

CAS No.
SMILES

O=C(N)C1=CC(F)=CC=C1C(C)(C)C[C@@](O)(CC(N2)=CC3=C2C=NC(S(=O)(CC)=O)=C3)C(F)(F)F

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BI 653048
Cat. No.:
HY-12946
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