BI-653048

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI 653048 phosphate 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 phosphate 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)。

An oral glucocorticoid agonist for the treatment of rheumatoid arthritis.Rheumatoid Arthritis Phase 1 Clinical.

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.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.BI 653048 phosphate inhibits TNF-stimulated IL-6 production in mouse RAW cells with an IC50 value of 100 nM.

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. Animal Model:Mice Dosage:3, 10, and 30 mg/kg Administration:Oral administrationResult:Exhibited significant decreases for all measured histology parameters at high doses.

BI653048 | BI 653048

Endocrinology/Hormones

GR

GR

Inflammation/Immunology

Rheumatoid Arthritis

1198784-97-2

613.517

C23H28F4N3O8PS

>98% (HPLC)

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O=C(N)C1=CC(F)=CC=C1C(C[C@@](O)(CC(N2)=CC3=C2C=NC(S(=O)(CC)=O)=C3)C(F)(F)F)(C)C.O=P(O)(O)O

(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

(-20℃)

With Ice Pack

≥ 2 years