Amlexanox (AA-673)

For research use only. Not for use in humans.

目录号:S3648 别名: CHX-3673, Amoxanox 中文名称:氨来占诺

Amlexanox (AA-673) Chemical Structure

CAS No. 68302-57-8

Amlexanox (AA-673, CHX-3673, Amoxanox)是一种抗炎抗过敏免疫调节剂,也是蛋白激酶 TBK1IKK-ε 的抑制剂。

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客户使用Selleck生产的Amlexanox (AA-673)发表文献8篇:

产品安全说明书

Immunology & Inflammation related抑制剂选择性比较

生物活性

产品描述 Amlexanox (AA-673, CHX-3673, Amoxanox)是一种抗炎抗过敏免疫调节剂,也是蛋白激酶 TBK1IKK-ε 的抑制剂。
靶点
TBK1 [1]
()
IKK-ε [1]
()
体外研究

Dose-response relationship of amlexanox inhibition of IKK-ɛ and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1-2 μM. Amlexanox also blocks the activity of TBK1 at approximately the same concentrations but has no effect on IKK-α or IKK-β and at these concentrations do not block any other kinases from a broad panel representing most kinase families. Inhibition of IKK-ɛ or TBK1 by amlexanox is competitive for its substrate ATP, indicating that it interacts with the enzymes in the ATP-binding site. Amlexanox increases the phosphorylation of TBK1 at 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 IKK-ɛ and TBK1[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ARPE-19 cells MWrGeY5kfGmxbjDhd5NigQ>? NUS3WGVtOSEQvF2= MmHXTY5pcWKrdHnvckBw\iCWQluxJIJ6KEGvbIigLFHjiIYEtV2pJJJm\HWlZYOgTGcucW6mdXPl[EBucXSxcHjh[4lkKG[udYi= NHHXT4w{OTB{M{[0OS=>
HCT-116 NYizRo9TTnWwY4Tpc44h[XO|YYm= NVTXd2pYOTByIN88US=> NYDSOmh2PDhiaB?= MXLBcYxmgGGwb4igd5RqdXWuYYTld{BmgHC{ZYPzbY9vKG[{b32gZUBPVURicnXwc5J1\XJidnXjeI9zNg>? MUOzNFcyQTF{Mh?=
PC3 MkfGSpVv[3Srb36gZZN{[Xl? NV3lOJp1OjBibl2sJFExOCCwTTygNe69VSCjbnSgOUDPxE1? MmrucIVi\HNidH:g[I9{[WenLXTldIVv\GWwdDDkc5dvemWpdXzheIlwdiCxZjDFUXQucW6mdXPpcochfHKjboPjdolxfGmxbnHsJIZi[3SxcoOgXoVjOSCjbnSgUk1k[WSqZYLpckwh[W6mIIXwdoVofWyjdHnvckBw\iCncHn0bIVtcWGuLYPw[YNq\mmlIIDyc5RmcW5iRT3jZYRp\XKrbh?= NVP1c|d4OzB{N{m3Nlg>
DU145 MX;GeY5kfGmxbjDhd5NigQ>? NIHCT3QzOCCwTTygNVAxKG6PLDCx{txOKGGwZDC1JO69VQ>? NXXOUXlZdGWjZIOgeI8h\G:|YXflMYRmeGWwZHXueEBld3ewcnXneYxifGmxbjDv[kBGVVRvaX7keYNqdmdidILhcpNkemmydHnvcoFtKG[jY4TvdpMhYmWkMTDhcoQhVi2lYXTo[ZJqdixiYX7kJJVxemWpdXzheIlwdiCxZjDldIl1cGWuaXHsMZNx\WOrZnnjJJBzd3SnaX6gSU1k[WSqZYLpci=> NWXqNpczOzB{N{m3Nlg>
U87 NVvLPW5CWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGHCd2oxNTNyMDFOwG0> M2G5VlI1NCB2ODygO|Ih[W6mIEm2JIg> MWjUbIUhUUN3MDD2ZYx2\XNiZn;yJFcz6oDLaDDv[kBidWyneHHuc5ghfHKnYYTt[Y51KHencnWgZZBxem:6aX3heIVtgSBzNEFihKnPxE1iaX6gWVg4KGOnbHzzMi=> NGTLRnYzQTB2OESzNC=>
U251 Mo\iVJJwdGmoZYLheIlwdiCjc4PhfS=> M{iyUVAuOzByIN88US=> MmLLNlQtKDR6LDC3NkBidmRiOU[gbC=> MlO4WIhmKEmFNUCgeoFtfWW|IH\vdkA4OuLCiXigc4Yh[W2uZYjhco95KHS{ZXH0cYVvfCC5ZYLlJIFxeHKxeHntZZRmdHliMUKw5qCK|ryPIHnuJHUzPTFiY3XscJMv MmDtNlkxPDh2M{C=
NIH 3T3 cells M3TjWGZ2dmO2aX;uJIF{e2G7 NYXK[IVpOSCvTTDvdkAxNjN5NTDtUS=> NUfIcm9pOjRiaB?= M1HHS2NmdGy|IHX4bIljcXSnZDDhJIRz[W2jdHnjJINp[W6pZTDpckB1cGWrcjDtc5JxcG:ub3f5JJRp[XRiaX7jcJVl\WRiYTDsZZJo\XJiYX7kJI1wemViZnzheJRmdmWmIIDo[Y5wfHmyZTDhcoQhd2[2ZX6g[Il{eGyjeXXkJIxwdmdicILvZ4V{e2W|IIToZZQh[XKnIIP0ZYJt\SCob4KgZZQhdGWjc4SgNVAh\GG7cx?= M3PVRVExQTJzOUGz
HUVEC NXvPN2lOTnWwY4Tpc44h[XO|YYm= MmDCNUBuVSCxcjCwMlM4PSCvTR?= NIjiS2ozPCCq MVztc4Rq\nliY3XscEBud3KyaH;sc4d6 NEXzeFgyODl{MUmxNy=>
Swiss 3T3 M17mRmZ2dmO2aX;uJIF{e2G7 M2PGfFEhdU1? NYC0[ldYOTBvM{[wJI1qdg>? M1;wU2FudGW6YX7vfEB4[XNiYXLs[UB1dyC|dHnteYxifGVidHjlJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBkd3K2YXP0bY4hcW5iYTDyZZBq\CCjbnSgd5V{fGGrbnXkJI1idm6ncj6= NFPFWJEyODl{MUmxNy=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
IKKε / TBK1 / IKKβ ; 

PubMed: 23396211     


Dose response of amlexanox inhibition of IKKε and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1-2 µM. Results were replicated in more than three experiments. 

MMP2 / MMP9 ; 

PubMed: 29048430     


The protein levels of MMP-2 and MMP-9 were evaluated by western blot. The results shown are representative of at least three independent experiments. Data are shown as the means±S.D. *P<0.05 and **P<0.01 compared with the control group

IKBKE / MST1 / MST2 / p-MST / LAST1 / LAST2 / p-YAP1 / YAP1 / Axl / c-Myc / Cyr61 ; 

PubMed: 29048430     


Amlexanox reduced the protein expression of the Hippo pathway through downregulation of IKBKE. (a) U87 and U251 cells were treated with various concentrations of amlexanox for 72 h. The cells were harvested, and the effects of amlexanox on the protein expression of the Hippo pathway were detected by western blot. (b) U87 and U251 cells were treated with amlexanox at 150 μM for 24, 48 and 72 h. Cell lysates were collected, and the protein expression were detected by western blot as in (a).

p-p65 / p-IκBα / S100A13 ; 

PubMed: 30670674     


HCT116 cells were treated with Dox (100 nM) for 4 days in the presence of the indicated doses of Amlexanox. Then, cell lysates were subjected to western blot analysis for the indicated proteins.

23396211 29048430 30670674
Growth inhibition assay
Cell viability; 

PubMed: 29048430     


(a and b) U87 and U251 cells were treated with amlexanox (0–300 μM) for 24, 48, 72 and 96 h, and cell vibility was detected using CCK-8 assay. 

29048430
体内研究 Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis[1].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: 3T3-L1 adipocytes
  • Concentrations: 12, 25, 50 μM
  • Incubation Time: 1 h
  • Method: TBK1 phosphorylation (pTBK1) at Ser172 and IRF3 phosphorylation at Ser396 (pIRF3) in 3T3-L1 adipocytes treated with amlexanox or cayman and with or without poly I:C are examined.
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: C57BL/6
  • Dosages: 25 or 100 mg per kg body weight
  • Administration: oral gavage
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 59 mg/mL (197.79 mM)
Water Insoluble
Ethanol '''1 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 298.29
化学式

C16H14N2O4

CAS号 68302-57-8
储存条件 粉状
溶于溶剂
别名 CHX-3673, Amoxanox

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

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 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

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 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID