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BI 653048

Catalog No.GC65345

BI 653048 is a selective and orally active nonsteroidal?glucocorticoid (GC)?agonist with an IC50 value of 55 nM.

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BI 653048 Chemical Structure

Cas No.: 1198784-72-3

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1mg
$405.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

CYP1A2

50μM(IC50)

CYP2D6

41μM(IC50)

CYP2C9

12μM(IC50)

CYP2C19

9μM(IC50)

CYP3A4

8μM(IC50)

Background

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].

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].

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].

[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

Chemical Properties

Cas No. 1198784-72-3 SDF Download SDF
Formula C23H25F4N3O4S M.Wt 515.52
Solubility Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9398 mL 9.6989 mL 19.3979 mL
5 mM 0.388 mL 1.9398 mL 3.8796 mL
10 mM 0.194 mL 0.9699 mL 1.9398 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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