AX-024

An inhibitor of the CD3ε-Nck interaction

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
2mg

￥900.00

720.00

- +
5mg

￥1337.00

1070.00

- +
10mg

￥2400.00

1920.00

- +
25mg

￥4712.00

3770.00

- +
50mg

￥8450.00

6760.00

- +
100mg

￥14962.00

11970.00

- +
200mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajce55122
CAS: 1370544-73-2
别名:
分子式: C21H22FNO2
分子量: 339.4
纯度: >98%
溶解度: Ethanol: 100 mg/mL (294.64 mM); DMSO: 35 mg/mL (103.12 mM and warming); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

AX-024 is an inhibitor of the CD3ε-Nck interaction.¹ 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 MOG_35-55 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).

1.Borroto, A., Reyes-Garau, D., Jiménez, M.A., et al.First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseasesSci. Transl. Med.8(370)370ra184(2016)

Protocol

Cell experiment:

Spleen B cells from C57BL/6 mice are labeled with Cell Trace Violet and incubated for 72 hours with either anti-IgM (10 mg/mL) or anti-CD40 (5 mg/mL), supplemented with IL-4 (5 ng/mL) or LPS (2.5 mg/mL) in the presence of different concentrations of AX-024. Proliferation is calculated according to the total number of cell divisions[1].

Animal experiment:

Eight-week-old CD-1 mice are injected intraperitoneally with different amounts of the AX-024 dissolved in 0.5 mL of saline. All animals are observed clinically for the appearance of macroscopically visible adverse reactions twice daily over 14 days, as well as immediately after AX-024 administration. A necropsy is carried out on each animal on day 14, and the abdominal, thoracic, and cranial cavities are examined in situ, together with their associated organs[1].

参考文献:

[1]. Borroto A, et al. First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases. Sci Transl Med. 2016 Dec 21;8(370):370ra184.