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BI 653048 phosphate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BI 653048 phosphate图片
CAS NO:1198784-97-2
包装:5 mg
市场价:7000元

产品介绍

产品描述

BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).

体外活性

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 inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM[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].

体内活性

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].

Cas No.

1198784-97-2

分子式

C23H28F4N3O8PS

分子量

613.52

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years