1206101-20-3 Usage
Description
GLPG0634, also known as N-[5-[4-[(6-Cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide, is an orally-available, selective inhibitor of JAK1 (Janus kinase 1). It is a promising pharmaceutical candidate with potential applications in the treatment of various inflammatory diseases, particularly rheumatoid arthritis.
Uses
Used in Pharmaceutical Industry:
GLPG0634 is used as an anti-inflammatory agent for the treatment of rheumatoid arthritis. It selectively inhibits JAK1, a key enzyme involved in the inflammatory response, thereby reducing inflammation and alleviating the symptoms of the disease.
Additionally, due to its potential to target other inflammatory pathways, GLPG0634 may also be used for the treatment of other inflammatory diseases. However, further research and clinical trials are necessary to confirm its efficacy and safety in these applications.
Biological Activity
glpg0634 is a potent and selective inhibitor of jak1 with ic50 values of 10, 28, 810 and 116 nm for jak1, jak2, jak3 and tyk2, respectively [1].janus kinase 1 (jak1) is a member of the jak family and is a non-receptor tyrosine kinase. jaks play an important role in the immune system. jak1 is a potential target for the treatment of immune-inflammatory diseases [1].glpg0634 is a potent and selective jak1 inhibitor. glpg0634 inhibited jak1, jak2, jak3 and tyk2 with ic50 values of 10, 28, 810 and 116 nm, respectively. in cd4+ t cells, glpg0634 significantly reduced il-6-induced stat1 phosphorylation with ic50 value of 629 nm, which suggested the inhibition of jak1. in cd33+ t cells, glpg0634 reduced gm-csf-induced stat5 phosphorylation with ic50 value of 17.5 μm, suggesting the inhibition of jak2. glpg0634 inhibited the differentiation of th1 and th2 cells mediated by il-4 and il-12, respectively. also, glpg0634 inhibited th17 differentiation induced by tgf-β, il-23, il-6 and il-1β [1].in rats, glpg0634 significantly reduced the mrna levels of mx2, which were modulated by ifn-α-jak1/tyk2 signaling. in collagen-induced arthritis (cia) rat model, glpg0634 significantly reduced the infiltration of inflammatory cells and reduced the levels of il-6, ip-10, xcl1 and mcp-1 [1].
references
[1]. van rompaey l, galien r, van der aar em, et al. preclinical characterization of glpg0634, a selective inhibitor of jak1, for the treatment of inflammatory diseases. j immunol, 2013, 191(7): 3568-3577.
Check Digit Verification of cas no
The CAS Registry Mumber 1206101-20-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,6,1,0 and 1 respectively; the second part has 2 digits, 2 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1206101-20:
(9*1)+(8*2)+(7*0)+(6*6)+(5*1)+(4*0)+(3*1)+(2*2)+(1*0)=73
73 % 10 = 3
So 1206101-20-3 is a valid CAS Registry Number.
1206101-20-3Relevant articles and documents
NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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Page/Page column 26, (2010/03/02)
A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn''s disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.
