2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Anti-infection
  3. Glucocorticoid Receptor Cytochrome P450 HCV Protease
  4. BI 653048 phosphate

BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate 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.

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BI 653048 phosphate Chemical Structure

BI 653048 phosphate Chemical Structure

CAS No. : 1198784-97-2

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BI 653048 phosphate Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM[1]. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM)[2]. BI 653048 phosphate 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[2]

CYP1A2

50 μM (IC50)

CYP2D6

41 μM (IC50)

CYP2C9

12 μM (IC50)

CYP2C19

9 μM (IC50)

CYP3A4

8 μM (IC50)

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 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 phosphate 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.

BI 653048 phosphate Related Antibodies
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].

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: Exhibited significant decreases for all measured histology parameters at high doses.
Clinical Trial
Molecular Weight

613.52

Formula

C23H28F4N3O8PS
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.O=P(O)(O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BI 653048 phosphate Related Classifications

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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.

Keywords:

BI 6530481198784-97-2BI653048BI-653048Glucocorticoid ReceptorCytochrome P450HCV ProteaseCYPsHCVNS3proteaseInhibitorinhibitorinhibit

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