| Identification | Back Directory | [Name]
AX-024 hydrochloride | [CAS]
1704801-24-0 | [Synonyms]
AX-024
AX-024;AX024;AX 024
AX-024 hydrochloride | [Molecular Formula]
C21H23ClFNO2 | [MDL Number]
MFCD31628548 | [MOL File]
1704801-24-0.mol | [Molecular Weight]
375.87 |
| Chemical Properties | Back Directory | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (10 mg/ml with warming). | [form ]
solid | [color ]
White | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
AX-024 is an inhibitor of the CD3ε-Nck interaction. It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC50 = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4+ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox). | [Uses]
AX-024 is a T cell receptor inhibitor for the treatment of autoimmune diseases. | [in vivo]
The AX-024 hydrochloride-treated group presents less scales and reduces skin thickening compare to the vehicle group. AX-024 hydrochloride significantly reduces thickening of both skin layers, but more effectively of the dermis, which rather resembles that of mice treated with a control cream lacking imiquimod (IMQ). AX-024 hydrochloride significantly diminishes the number of airway inflammatory cells in both assays. Mice receiving AX-024 hydrochloride rapidly recovers from neurological impairment and weight loss, becoming symptom-free by day 30, unlike mice that receives the vehicle, in which ataxia and loss of the righting reflex persist[1]. | [IC 50]
IL-6; IL-10; IL-17A | [References]
1) Borroto et al. (2016), First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases; Sci. Transl. Med., 8 370ra184 |
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| Company Name: |
Twochem Co.Ltd.
|
| Telephone: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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