| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:BI 653048 phosphate
CAS:1198784-97-2
Package:25mg/RMB 26100
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| | BI 653048) Basic information |
| | BI 653048) Chemical Properties |
| | BI 653048) Usage And Synthesis |
| Uses | BI 653048 phosphate is a selective and orally active nonsteroidalglucocorticoid (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 aHCV NS3 proteaseinhibitor that can reduce viral loads infected with thehepatitis Cvirus[3]. | | 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. |
| | IC 50 | CYP1A2: 50 μM (IC50); CYP2D6: 41 μM (IC50); CYP2C9: 12 μM (IC50); CYP2C19: 9 μM (IC50); CYP3A4: 8 μM (IC50) | | 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. DOI:10.1021/jo400079z
[2] Harcken C, et al. Optimizationofdrug-likepropertiesofnonsteroidalglucocorticoidmimeticsandidentificationof aclinicalcandidate.ACS Med Chem Lett.2014 Nov 20;5(12):1318-23. DOI:10.1021/ml500387y
[3] Montse Llinas-Brunet, et al. Latest bibliographic data on file with the International Bureau |
| | BI 653048) Preparation Products And Raw materials |
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