1. GPCR/G Protein
    Metabolic Enzyme/Protease
  2. Glucocorticoid Receptor
    Cytochrome P450
    HCV Protease
  3. BI 653048 phosphate

BI 653048 phosphate 

Cat. No.: HY-12946A
Handling Instructions

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.

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

BI 653048 phosphate Chemical Structure

BI 653048 phosphate Chemical Structure

CAS No. : 1198784-97-2

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of BI 653048 phosphate:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

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].

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].

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.

1198784-97-2

SMILES

O=C(N)C1=CC(F)=CC=C1C(C)(C)C[[email protected]@](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.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BI 653048BI653048BI-653048Glucocorticoid ReceptorCytochrome P450HCV ProteaseCYPsHCVNS3proteaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
BI 653048 phosphate
Cat. No.:
HY-12946A
Quantity:
MCE Japan Authorized Agent: