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AX-024 hydrochloride

产品编号 T4403 CAS 1704801-24-0

别名: AX-024 HCl

AX-024 hydrochloride (AX-024 HCl) 是一种细胞因子释放抑制剂，可强烈抑制 IL-6、TNFα、IFN-γ、IL-10 和 IL-17A 的产生。它是口服可利用的 TCR-Nck 相互作用抑制剂，可选择性地抑制 TCR 触发的 T 细胞活化。它通过靶向 SH3结构域调节细胞信号传导，具有低毒、高效和高选择性的特点。

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AX-024 hydrochloride, CAS 1704801-24-0

规格	价格/CNY	货期
1 mg	￥ 378	现货
2 mg	￥ 549	现货
5 mg	￥ 892	现货
10 mg	￥ 1,490	现货
25 mg	￥ 1,980	现货
50 mg	￥ 3,480	现货
100 mg	￥ 5,130	现货
1 mL * 10 mM (in DMSO)	￥ 981	现货

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其他形式的 AX-024 hydrochloride:

AX-024
询价

选择批次

纯度: 99.9%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	AX-024 hydrochloride (AX-024 HCl) is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.
体外活性	Compound AX-024 hydrochloride is >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 hydrochloride in this assay is 1 nM, although it shows inhibitory effects at a concentration of 1 pM or less. AX-024 hydrochloride is 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 necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10, and IL-17A production at a concentration of 10 nM. In CD8+ T cells of OT1 TCR transgenic (OT1Tg) mice bearing wild-type (WT) AX-024 hydrochloride strongly inhibits T cell proliferation at a concentration of 0.1 nM when OT1Tg T cells are WT for the PRS mutation. Coimmunoprecipitation experiments in these cells show that Nck recruitment to the TCR is induced upon stimulation in the absence of drug but is inhibited in the presence of AX-024 hydrochloride in a dose-dependent manner at concentrations starting from 1 nM.
体内活性	The AX-024 hydrochloride-treated group presents less scales and reduces skin thickening compare to the vehicle group. Treatment with 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). Treatment with 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.
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 hydrochloride. Proliferation is calculated according to the total number of cell divisions. They are for reference only.
动物实验	Eight-week-old CD-1 mice are injected intraperitoneally with different amounts of the AX-024 hydrochloride 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 hydrochloride 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. They are for reference only.

别名	AX-024 HCl
分子量	375.87
分子式	C21H23ClFNO2
CAS No.	1704801-24-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 33 mg/mL

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参考文献

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

文献引用

1. Li Y, Lai J, Ran M, et al.Alnustone promotes megakaryocyte differentiation and platelet production via the interleukin-17A/interleukin-17A receptor/Src/RAC1/MEK/ERK signaling pathway.European Journal of Pharmacology.2024: 176548.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AX-024 hydrochloride 1704801-24-0 Apoptosis Immunology/Inflammation Neuroscience IL Receptor TNF COX IFNAR Interleukin AX 024 Interleukin Related Inhibitor AX024 Hydrochloride inhibit Tumor Necrosis Factor Receptor AX024 hydrochloride AX 024 Hydrochloride AX-024 HCl TNFR Interferon-α/β receptor AX024 AX-024 AX-024 Hydrochloride TNF Receptor AX 024 hydrochloride Interferon-alpha/beta receptor inhibitor

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AX-024 hydrochloride

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