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

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BI 653048 Chemical Structure

BI 653048 Chemical Structure

CAS No. : 1198784-72-3

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1 mg USD 450 In-stock
5 mg USD 1800 In-stock
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100 mg USD 14800 In-stock
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Based on 1 publication(s) in Google Scholar

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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[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 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.

BI 653048 Related Antibodies
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.
Unlabeled Cas

Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9398 mL 9.6989 mL 19.3979 mL
5 mM 0.3880 mL 1.9398 mL 3.8796 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9398 mL 9.6989 mL 19.3979 mL 48.4947 mL
5 mM 0.3880 mL 1.9398 mL 3.8796 mL 9.6989 mL
10 mM 0.1940 mL 0.9699 mL 1.9398 mL 4.8495 mL
15 mM 0.1293 mL 0.6466 mL 1.2932 mL 3.2330 mL
20 mM 0.0970 mL 0.4849 mL 0.9699 mL 2.4247 mL
25 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
30 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6165 mL
40 mM 0.0485 mL 0.2425 mL 0.4849 mL 1.2124 mL
50 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
60 mM 0.0323 mL 0.1616 mL 0.3233 mL 0.8082 mL
80 mM 0.0242 mL 0.1212 mL 0.2425 mL 0.6062 mL
100 mM 0.0194 mL 0.0970 mL 0.1940 mL 0.4849 mL
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BI 653048 Related Classifications

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 6530481198784-72-3BI653048BI-653048Glucocorticoid ReceptorCytochrome P450HCV ProteaseCYPsHCVNS3proteaseInhibitorinhibitorinhibit

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