| 中文名称: | Amlexanox | ||||
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| 英文名称: | Amlexanox | ||||
| 别名: | 2-氨基-7-异丙基-5-氧代-5H-苯并吡喃并[2,3-b]吡啶-3-羧酸;氨来呫诺 2-Amino-7-isopropyl-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid | ||||
| CAS No: | 68302-57-8 | 分子式: | C16H14N2O4 | 分子量: | 298.29 |
| CAS No: | 68302-57-8 | ||||
| 分子式: | C16H14N2O4 | ||||
| 分子量: | 298.29 | ||||
| EINEC: | 2686 | ||||
| EINEC: | 2686 | ||||
基本信息
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产品编号： |
A70348 |
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产品名称： |
Amlexanox |
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CAS: |
68302-57-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
298.29 |
-20℃ |
1个月 |
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化学名： |
2-Amino-7-isopropyl-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid |
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Solubility (25°C)： |
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体外:
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DMSO |
60mg/mL (201.14mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照In Vitro⽅式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐是指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶 1.请依序添加每种溶剂：0.5% CMC-Na/saline water Solubility:20mg/mL(67.05mM);Suspended solution;Need ultrasonic 2.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(8.38mM);Clear solution 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(8.38mM);Clear solution |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.3524mL |
16.7622mL |
33.5244mL |
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5mM |
0.6705mL |
3.3524mL |
6.7049mL |
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10mM |
0.3352mL |
1.6762mL |
3.3524mL |
生物活性
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产品描述 |
一种特异性的IKKε和TBK1抑制剂，IC50值为1-2μM。 |
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靶点 |
IKKε 1-2μM (IC50) |
TBK1 1-2μM (IC50) |
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体外研究 |
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.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.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-κ B (NF-κB),mitogen-activated protein kinase (MAPKs),c-Fos and NFATc1. Amlexanox decreases the expression of osteoclastspecific genes, including TRAP,MMP9,Cathepsin K and NFATc1. |
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体内研究 |
Amlexanox (100mg/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 (25mg/kg) significantly improves insulin sensitivity in mice with established DIO,and after four weeks of treatment,amlexanox produces marked improvements in glucose.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.Amlexanox (20mg/kg) enhances osteoblast differentiation of BMSCs.In ovariectomized (OVX) mouse model,amlexanox prevents OVX-induced bone loss by suppressing osteoclast activity. |
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推荐实验方法(仅供参考)
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激酶实验： |
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The in vitro kinase assays is performed by incubating purified kinase (IKKε or TBK1) in kinase buffer containing 25mM Tris (pH7.5),10mM MgCl2,1mM DTT,and 10µM ATP for 30 minutes at 30℃ in the presence of 0.5µCi γ-[32P]-ATP and 1µg 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℃.Supernatants are resolved by SDS-polyacrylamide gel electrophoresis,transferred to nitrocellulose,and analyzed by autoradiography using a Typhoon 9410 phosphorimager. |
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细胞实验: |
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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 (0,1.5,3,6,12,25μM) every 2 days in the presence of M-CSF (30ng/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℃ for an additional 2h.The absorbance is then measured at a wavelength of 450nm on an ELX800 absorbance microplate reader. |
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动物实验: |
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Wildtype male C57BL/6 mice are fed with a HFD consisting of 45% of calories from fat starting at eight weeks of age for 12-24 weeks,while ND C57BL/6 controls are maintained on normal chow diet consisting of 4.5% fat.C57BL/6 diets are fed containing ω-3 fatty acids.Rosiglitazone treatment is administered for three weeks by addition of the compound to the diet in mice that have been on HFD for 16 weeks.Each mouse consumes on average 3.5mg per kg rosiglitazone per day.AmLexanox is administered by daily oral gavage.For the prevention groups,amLexanox (25mg per kg or 100mg per kg) administration is begun concurrently with HFD feeding at eight weeks of age.For the treatment groups,25mg per kg amLexanox treatment is begun at 20 weeks of age after 12 weeks of HFD.To test the effect of amLexanox withdrawal,mice in the treatment group are switched from amLexanox gavage to vehicle control after eight weeks of amLexanox treatment.Control and ob/ob mice are fed with a normal chow diet and gavaged with 100mg per kg amLexanox or vehicle control beginning at ten weeks of age.Animals are housed in a specific pathogen-free facility with a 12-hour light/12-hour dark cycle and given free access to food and water. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
