Shanghai Nianxing Industrial Co., Ltd
China
Product Name: BI 653048 phosphate
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Purity: 98.0%
Stocking Period: 10 Day
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ShangHai DC Chemicals Co.,Ltd
China
Product Name: BI-653048
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai
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DC Chemicals Limited
China
Product Name: BI-653048
Price: $Inquiry/25mg $Inquiry/100mg $Inquiry/500mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

1198784-97-2

1198784-97-2 structure

1198784-97-2 structure

Name: BI 653048 phosphate
Chemical Name: BI-653048
CAS Number: 1198784-97-2
Molecular Formula: C₂₃H₂₈F₄N₃O₈PS
Molecular Weight: 613.517
Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
Create Date: 2020-01-20 17:22:57
Modify Date: 2024-01-10 06:41:56
An oral glucocorticoid agonist for the treatment of rheumatoid arthritis. Rheumatoid Arthritis Phase 1 Clinical

Name	BI-653048

Description	An oral glucocorticoid agonist for the treatment of rheumatoid arthritis. Rheumatoid Arthritis Phase 1 Clinical
Related Catalog	Research Areas >> Infection Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Signaling Pathways >> Metabolic Enzyme/Protease >> HCV Protease Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor
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.
References	[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

Molecular Formula	C₂₃H₂₈F₄N₃O₈PS
Molecular Weight	613.517

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