BI 653048 phosphate 

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].

BI 653048 phosphate 表现出增强的类药物特性，抑制 CP1A2、CYP2D6、CYP2C9、CYP2C19 和 CYP3A4，IC₅₀ 值分别为 50 μM、41 μM、12 μM、9 μM 和 8 μM^[2]。
BI 653048 phosphate 可降低对 hERG 离子通道的亲和力，在表达人类 ERG 钾通道的重组 HEK293 细胞中，IC₅₀>30 μM^[2]。
BI 653048 phosphate 可抑制 TNF 刺激的小鼠 RAW 细胞中 IL-6 的产生，IC₅₀ 值为 100 nM^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BI 653048 (口服给药；3、10 和 30 mg/kg) phosphate 在 3 mg/kg 剂量下，所有测量的组织学参数 (踝关节炎症、血管翳形成、软骨损伤和骨吸收) 均未显著降低。中剂量 (10 mg/kg) 治疗显著降低血管翳和骨吸收 (33%) 以及总评分 (27%)，而高剂量 (30 mg/kg) 治疗则显著降低所有参数 (87-96%)。总评分的 ED₅₀ 值为 14 mg/kg^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

613.52

C₂₃H₂₈F₄N₃O₈PS

1198784-97-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. Montse Llinas-Brunet, et al. Latest bibliographic data on file with the International Bureau