AX-024, ≥98%
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| CAS | 1370544-73-2 |
|---|---|
| 英文名称 | AX-024 |
| 别名 | AX-024 HCl |
| 纯度 | ≥98% |
| 分子量 | 339.4 |
| 外观（性状） | Liquid |
| 储存条件 | 2-8℃, 2 years |
| 溶解性 | Soluble in DMSO |
| MDL | MFCD30609505 |
| InChIKey | VMMKGVRPILDZML-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H22FNO2/c1-24-18-8-9-20-19(12-18)21(15-4-6-17(22)7-5-15)16(14-25-20)13-23-10-2-3-11-23/h4-9,12H,2-3,10-11,13-14H2,1H3 |
| PubChem CID | 56949412 |
| 货期 | 1-2天 |
| SMILES | COC1=CC=C(OC2)C(C(C3=CC=C(F)C=C3)=C2CN4CCCC4)=C1 |
| 描述 | AX-024特异性地抑制TCR依赖性的T细胞激活。AX-024特异性地抑制早期TCR信号传导。对IL-6、TNF-α、IFN-γ、IL-10和IL-17A的产生有很强的抑制作用。(AX-024 specifically inhibits TCR-dependent T cell activation.AX-024 specifically inhibits the earliest TCR signaling events.It has a strong inhibitory effect on the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.) |
| 靶点 | TCR;IFNAR；Interleukin Related |
| 通路 | Immunology & Inflammation |
| 生物活性 | AX-024 specifically inhibits TCR-dependent T cell activation.AX-024 specifically inhibits the earliest TCR signaling events.AX-024 attenuates the severity of skin inflammation in a psoriasis model as well as of lung inflammation in an asthma model.[1] |
| In Vitro | Replacing the piperidine substituent by a smaller pyrrolidine ring and adding a methoxy substituent in position 6 gave rise to the lead compound AX-024, which was >10,000-fold more potent than the AX-000 hit in terms of inhibition of TCR-triggered T cell proliferation. The IC50 of AX-024 in this assay was 1 nM, although it showed inhibitory effects at a concentration of 1 pM or less. AX-024 was also a much more potent inhibitor of cytokine release by human peripheral blood mononuclear cells stimulated with anti-CD3 than AX-000, strongly hindering interleukin-6 (IL-6),tumor necrosisfactor–a (TNFa), interferon-g (IFN-g), IL-10, and IL-17A production at a concentration of 10 nM.[1] |
| In Vivo | AX-024-treated group presents less scales and reduces skin thickening compare to the vehicle group. AX-024 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 significantly diminishes the number of airway inflammatory cells in both assays. Mice receiving AX-024 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 数据来源文献 | [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 |
| 规格 | 5mg10mg |
| 单位 | 瓶 |
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