产品名称

Filgotinib (GLPG0634)

一般描述

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

别 称

N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

纯 度

≥98.5%(HPLC)

CAS NO.

1206161-97-8

分子式

C²¹H²³N⁵O³S

分子量

425.5

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥50mg/ml

乙醇

Insoluble

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Filgotinib is an orally bioavailable inhibitor of the tyrosine kinase Janus kinase 1 (JAK1), with potential anti-inflammatory and immunomodulating activities. Upon oral administration, filgotinib specifically targets, binds to, and inhibits the phosphorylation of JAK1, which interferes with JAK/STAT (signal transducer and activator of tranion)-dependent signaling. As JAK1 mediates signaling of many pro-inflammatory cytokines, JAK1 inhibition prevents cytokine signaling and activity in many inflammatory and immune-mediated processes and leads to a decrease in inflammation and activation of certain immune cells. JAK1 plays a key role in the signaling and activity of many cytokines and growth factors and is often dysregulated in a variety of autoimmune and inflammatory diseases, as well as some malignancies.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov