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Amlexanox

Amlexanox

产品编号 T1639   CAS 68302-57-8
别名: 氨来呫诺, CHX3673, Amoxanox, 氨来诺, AA673

Amlexanox (AA673) 是一种特异性的 IKKε和 TBK1抑制剂,其 IC50=1-2 μM。

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Amlexanox Chemical Structure
Amlexanox, CAS 68302-57-8
规格 价格/CNY 货期 数量
5 mg ¥ 285 现货
25 mg ¥ 453 现货
50 mg ¥ 663 现货
100 mg ¥ 828 现货
500 mg ¥ 1,980 现货
1 mL * 10 mM (in DMSO) ¥ 410 现货
产品目录号及名称: Amlexanox (T1639)
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纯度: 100%
纯度: 99.56%
纯度: 99.55%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.
靶点活性 TBK1:1-2 μM, IKKε:1-2 μM
体外活性 AmLexanox increases phosphorylation of TBK1 on Ser172 in 3T3-L1 adipocytes, and blocks polyinosinic:polycytidylic acid (poly I:C)-stimulated phosphorylation of interferon responsive factor-3 (IRF3), a presumed substrate of IKKε and TBK1[1]. AmLexanox potently inhibits the release of histamine and leukotrienes from mast cells, basophils and neutrophils in in vitro settings, possibly through increasing intracellular cyclic AMP content in inflammatory cells, a mem-brane-stabilising effect or inhibition of calcium influx[2]. In primary bone marrow derived macrophages (BMMs), amLexanox inhibits osteoclast formation and bone resorption. At the molecular level, amLexanox suppresses RANKL-induced activation of nuclear factor-κB (NF-κB), mitogen-activated protein kinase (MAPKs), c-Fos and NFATc1. AmLexanox decreases the expression of osteoclast-specific genes, including TRAP, MMP9, Cathepsin K and NFATc1[3].
体内活性 AmLexanox (100 mg/kg, p.o.) prevents and reverses diet-induced or genetic obesity, and produces reversible weight loss in obese mice. AmLexanox also causes a significant decrease in adipose tissue mass in these mice, and an increase in circulating adiponectin. AmLexanox (25 mg/kg) significantly improves insulin sensitivity in mice with established DIO,and after four weeks of treatment, amLexanox produces marked improvements in glucose[1]. AmLexanox before the first application of the paste and at each has been shown to suppress both immediate and evaluation thereafter. A categorical scale is also delayed-type hypersensitivity reactions[2]. AmLexanox (20?mg/kg) enhances osteoblast differentiation of BMSCs. In ovariectomized (OVX) mouse model, amLexanox prevents OVX-induced bone loss by suppressing osteoclast activity[3].
激酶实验 The in vitro kinase assays is performed by incubating purified kinase (IKKε or TBK1) in kinase buffer containing 25 mM Tris (pH7.5), 10 mM MgCl2, 1 mM DTT, and 10 μM ATP for 30 minutes at 30°C in the presence of 0.5 μCi γ-[32P]-ATP and 1 μg MBP per sample as a substrate. The kinase reaction is stopped by adding 4x sodium dodecyl sulfate (SDS) sample buffer and boiling for 5 minutes at 95°C. Supernatants are resolved by SDS-polyacrylamide gel electrophoresis, transferred to nitrocellulose, and analyzed by autoradiography using a Typhoon 9410 phosphorimager.
细胞实验 To examine cell proliferation, a Cell Counting Kit-8 is used according to the manufacturer's instructions. BMMs are seeded at a density of 5×103 cells/well in 96-well plates. After 24?hours, cells are treated with different concentrations of AmLexanox (0, 1.5, 3, 6, 12, 25?μM) every 2 days in the presence of M-CSF (30?ng/mL) for 7 days. After 1, 3, 5 and 7 days, the culture medium is replaced by the medium containing 10% CCK-8 and cells are incubated at 37°C for an additional 2?h. The absorbance is then measured at a wavelength of 450?nm on an ELX800 absorbance microplate reader.
别名 氨来呫诺, CHX3673, Amoxanox, 氨来诺, AA673
分子量 298.29
分子式 C16H14N2O4
CAS No. 68302-57-8

存储

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

溶解度

DMSO: 29.8 mg/mL(100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3524 mL 16.7622 mL 33.5244 mL 83.8111 mL
5 mM 0.6705 mL 3.3524 mL 6.7049 mL 16.7622 mL
10 mM 0.3352 mL 1.6762 mL 3.3524 mL 8.3811 mL
20 mM 0.1676 mL 0.8381 mL 1.6762 mL 4.1906 mL
50 mM 0.067 mL 0.3352 mL 0.6705 mL 1.6762 mL
100 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8381 mL

计算器

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参考文献

1. Reilly SM, et al. An inhibitor of the protein kinases TBK1 and IKK-e improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21. 2. Bell, J. AmLexanox for the treatment of recurrent aphthous ulcers. Clin Drug Investig, 2005. 25(9): p. 555-66. 3. Zhang Y, et al. AmLexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575. 4. Cheng, Chaping, et al. Aphthous ulcer drug inhibits prostate tumor metastasis by targeting IKKɛ/TBK1/NF-κB signaling [J]. Theranostics. 2018 Sep 9;8(17):4633-4648.

文献引用

1. Cheng C, Ji Z, Sheng Y, et al. Aphthous ulcer drug inhibits prostate tumor metastasis by targeting IKKɛ/TBK1/NF-κB signaling. Theranostics. 2018, 8(17): 4633
Brodalumab Ac-YVAD-CMK Anti-inflammatory agent 42 Kansuinine A Britannilactone diacetate RO2959 Hydrochloride Heliangin Corydine

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌上市药物库 酪氨酸激酶分子库 抗纤维化化合物库 临床期小分子药物库 免疫/炎症分子化合物库 抗肺癌化合物库 激酶抑制剂库 成骨分子库

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
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g
给药体积
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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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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

Amlexanox 68302-57-8 Angiogenesis Immunology/Inflammation NF-Κb Others Tyrosine Kinase/Adaptors IL Receptor FGFR IκB/IKK 氨来呫诺 CHX-3673 AA 673 I kappa B kinase inhibit IKK Inhibitor CHX3673 IκB kinase Amoxanox 氨来诺 CHX 3673 AA-673 AA673 inhibitor

 

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