Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AX-024 is a novel chemical compound that acts as an orally available inhibitor of the TCR-Nck interaction. Its primary mechanism of action is the selective inhibition of T cell activation triggered by TCR stimulation. With an IC50 value of approximately 1 nM, AX-024 effectively modulates cell signaling by specifically targeting SH3 domains. Additionally, AX-024 demonstrates desirable characteristics such as low acute toxicity, high potency, and excellent selectivity. Notably, it exhibits strong inhibitory effects on the production of IL-6, TNF-α, IFN-γ, IL-10, and IL-17A. 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 AX-024 hydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 692 | 5日内发货 | ||
5 mg | ¥ 1,260 | 6-8周 | ||
100 mg | ¥ 11,600 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,280 | 6-8周 |
AX-024 的其他形式现货产品:
产品描述 | AX-024 is a novel chemical compound that acts as an orally available inhibitor of the TCR-Nck interaction. Its primary mechanism of action is the selective inhibition of T cell activation triggered by TCR stimulation. With an IC50 value of approximately 1 nM, AX-024 effectively modulates cell signaling by specifically targeting SH3 domains. Additionally, AX-024 demonstrates desirable characteristics such as low acute toxicity, high potency, and excellent selectivity. Notably, it exhibits strong inhibitory effects on the production of IL-6, TNF-α, IFN-γ, IL-10, and IL-17A. |
体外活性 | AX-024 is >10,000-fold more potent than the AX-000 hit in terms of inhibition of TCR-triggered T cell proliferation. The IC 50 of AX-024 in this assay is 1 nM, although it shows inhibitory effects at a concentration of 1 pM or less. AX-024 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 (TNF-α), interferon-γ (IFN-γ), IL-10, and IL-17A production at a concentration of 10 nM. In CD8 + T cells of OT1 TCR transgenic (OT1 Tg ) mice bearing wild-type (WT) AX-024 strongly inhibits T cell proliferation at a concentration of 0.1 nM when OT1 Tg 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 in a dose-dependent manner at concentrations starting from 1 nM [1]. |
体内活性 | 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]. |
分子量 | 339.4 |
分子式 | C21H22FNO2 |
CAS No. | 1370544-73-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
AX-024 1370544-73-2 Inhibitor inhibitor inhibit