AX-024, Inhibits TCR-dependent T cell activation (TBI4895)

Description

Product Details

Formal Name: 1-[[4-(4-Fluorophenyl)-6-methoxy-2H-chromen-3-yl]methyl]pyrrolidine hydrochloride

Molecular Formula: C₂₁H₂₂FNO₂·HCl

Formula Weight: 375.86

CAS Number: 1704801-24-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (up to 10 mg/ml with warming)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Inhibits TCR-dependent T cell activation

Functions

Potent (IC50 ~ 1 nM) and specific inhibitor of T cell antigen receptor (TCR)-dependent T cell activation. Does not inhibit B cell proliferation triggered by B cell antigen receptor (BCR), TLR4, CD40 agonists nor IL-2-dependent proliferation of T lymphoblasts. Binds to the SH3.1 domain of the adaptor protein Nck blocking its interaction with the CD3ε subunit on the T cell antigen receptor. AX-024 displays protective effects in mouse models of psoriasis, allergic asthma, and multiple sclerosis. In contrast to fingolimod, the therapeutic effect of AX-024 persisted after removal of the drug, suggesting a persistent modification of autoimmune T cells. Currently in clinical trials.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml with warming) or in Water (up to 10 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.