Chemical Name: 1-[[4-(4-Fluorophenyl)-6-methoxy-2H-chromen-3-yl]methyl]pyrrolidine hydrochloride
T cell antigen receptor (TCR)-dependent T cell activation inhibitor
Molekulargewicht:
375.86
Reinheit:
98% by HPLC NMR (Conforms)
Formulierung:
White solid
CAS Nummer:
[1704801-24-0]
Formel:
C21H22FNO2HCl
Anwendungsbeschreibung:
AX-024 is a potent (IC50 ~ 1 nM) and specific inhibitor of T cell antigen receptor (TCR)-dependent T cell activation. It inhibited neither B cell proliferation triggered by B cell antigen receptor (BCR), TLR4, CD40 agonists nor IL-2-dependent proliferation of T lymphoblasts. AX-024 binds to the SH3.1 domain of the adaptor protein Nck blocking its interaction with the CD3 subunit on the T cell antigen receptor. AX-024 displayed protective effects in mouse models of psoriasis, allergic asthma, and multiple sclerosis. Importantly, the therapeutic effect of AX-024 persisted after removal of the drug in contrast to fingolimod suggesting a persistent modification of autoimmune T cells. Currently in clinical trials.
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