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- CAS号：
1704801-24-0
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥303.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥602.0 |
| 规格： | 5mg | 产品价格： | ￥677.0 |
| 规格： | 10mg | 产品价格： | ￥1128.0 |
| 规格： | 25mg | 产品价格： | ￥1504.0 |
| 规格： | 50mg | 产品价格： | ￥2640.0 |
| 规格： | 100mg | 产品价格： | ￥3896.0 |
| 规格： | 200mg | 产品价格： | ￥5504.0 |
Product Introduction
Bioactivity
| 名称 | AX-024 hydrochloride |
| 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. |
| 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. |
| 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 45 mg/mL (119.72 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2 mg/mL (5.32 mM), Sonication is recommended. |
| 关键字 | Tumor Necrosis Factor Receptor | TNF-α | TNFR | TNF Receptor | Interleukin Related | Interleukin | Interferon-α/β receptor | Interferon-alpha/beta receptor | Inhibitor | inhibit | ILReceptor | IL-6 | IL-17A | IL-10 | IL Receptor | IFN-γ | IFNAR | AX-024 Hydrochloride | AX024 Hydrochloride | AX-024 | AX024 | AX 024 Hydrochloride | AX 024 |
| 相关产品 | Trometamol | Rhamnose monohydrate | Kaolin | 1,4-Naphthoquinone | Glucosamine | Gum arabic | Acetaminophen | Tributyrin | Gluconate Calcium | 1,8-Cineole | D(+)-Raffinose pentahydrate | Hydroxypropyl Cellulose |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Anti-Aging Compound Library | Membrane Protein-targeted Compound Library | Anti-Neurodegenerative Disease Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Pain-Related Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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相关实验
620-gPRDX1 和 SW620-gNS 细胞进行裸鼠成瘤，来评估 PRDX1 敲低对这些化合物抗肿瘤功效的影响。当肿瘤生长到 50mm 时，小鼠用雷公藤红素和 19-048 进行治疗，结果表明雷公藤红素和 19-048 抑制了 SW620-gNS 肿瘤的进展。同时，作者对小鼠进行了毒性试验，结果表明，与雷公藤红素相比，19-048 在体内的安全性显著提高。免疫组织化学染色显示，在 SW620-gNS 移植小鼠中，随着雷公藤红素和 19-048 处理，GADD45G 和γ-H2AX 蛋白水平升高
的 相互作用，并充当效应蛋白的平台，导致下游级联事件。 磷酸化发生在所有核心组蛋白上，并且对每一个核心组蛋白都有不同的作用。组蛋白 H3 在丝氨酸 10 和 28 上的磷酸化，以及组蛋白 H2A 在 T120 上的磷酸化参与了染色质致密化以及有丝分裂过程中 染色质结构和功能的调节。这些是细胞周期和细胞生长的重要标志，在真核生物中得以保留。S139 处 H2AX 的磷酸化（产生 γH2AX）作为 DNA 损伤修复蛋白的招募点 (Lowndes et al., 2005, Pinto et al
润滑脂、纤维润滑脂、石墨润滑脂 3、库伦滴定 阳极液：Aquamicron® AXI(AX or AS) 100ml 阴极液：Aquamicron® CXU 5ml 检测对象：汽油、石脑油（粗汽油）、煤油、重油、轧制油、航空油、制冷机油、驱动油、制动液、液体石蜡、电气绝缘油、烷基苯 4、库伦滴定-水分挥发(加热到110-150℃) 阳极液：Aquamicron® AXI(AX or AS) 150ml 阴极液：Aquamicron® CXU 10ml 检测
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化合物 AX-024 HCl【1704801-24-0】
￥303 - 5504
