BI 653048|1198784-72-3|-陌孚医药/Medlife

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BI 653048

目录号: PL03052

CAS No. :1198784-72-3

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中文名称	BI 653048
英文名称	BI 653048
英文别名	BI 653048 (phosphate);(R)-2-(4-((5-(Ethylsulfonyl)-1H-pyrrolo[2,3-c]pyridin-2-yl)methyl)-5,5,5-trifluoro-4-hydroxy-2-methylpentan-2-yl)-5-fluorobenzamide phosphate;BI 653048
Cas No.	1198784-72-3
分子式	C₂₃H₂₈F₄N₃O₈PS
分子量	613.52
包装储存	Please store the product under the recommended conditions in the Certificate of Analysis.

产品详情

BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂，其 IC₅₀ 值为 55 nM。BI 653048 抑制 CP1A2，CYP2D6，CYP2C9，CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC₅₀>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103)，它也是一种 HCV NS3 protease 抑制剂，可以减少感染丙型肝炎病毒的病毒载量。

生物活性

BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC 50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC 50 >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.

IC50 & Target[1][2]

CYP1A2 50 μM (IC50) CYP2D6 41 μM (IC5

体外研究(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.
BI 653048 reduces affinity for the hERG ion channel with an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel.
BI 653048 inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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 ED 50 value for the summed scores is 14 mg/kg.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

ClinicalTrial

参考文献

[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.

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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