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氨来呫诺, 磷酸二酯酶 4 抑制剂

选择性TBK1和IKKε抑制剂
COA COA
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
A136009-250mg
 250mg 现货 Stock Image
A136009-1g
 1g 现货 Stock Image
A136009-5g
 5g 现货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
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IKK (58) inhibitor of nuclear factor kappa B kinase subunit epsilon Inhibitor (10) NF-κB (756) TANK binding kinase 1 Inhibitor (14)
main product photo

基本描述

别名 2-氨基-7-异丙基-5-氧代色满[2,3-b]吡啶-3-甲酸
英文别名 AMLEXANOX (MART.) | CHX 3673 | OraDisc A | ANW | aphtheal | US10214536, Amlexanox | Amlexanox- Bio-X | 2-Amino-7-isopropyl-5-oxo-5H-(1)benzopyrano(2,3-b)pyridine-3-carboxylic acid | 2-Amino-7-isopropyl-5-oxo-5H-[1]benzopyrano[2,3-b] pyridine-3-carboxylic
规格或纯度 Moligand™, ≥98%(HPLC)
英文名称 Amlexanox
生化机理 选择性TBK1和IKKε抑制剂（IC 50 = 1-2μM）。在体内显示出抗过敏，抗肥胖和抗炎作用。口服具有活性
储存温度 -20°C储存,充氩
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 磷酸二酯酶 4 抑制剂
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
纯度 ≥98%(HPLC)

产品属性

ALogP 3.1

关联靶点（人）

IKBKE Tchem 核因子 κB 激酶亚基 ε 抑制剂(Inhibitor of nuclear factor kappa-B kinase subunit epsilon) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
TBK1 Tchem 丝氨酸/苏氨酸蛋白激酶 TBK1(Serine/threonine-protein kinase TBK1) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
VDR Tclin Vitamin D receptor (26531 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BDKRB2 Tclin Bradykinin B2 receptor (3970 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRNA4 Tclin Neuronal acetylcholine receptor protein alpha-4 subunit (1265 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ttr Transthyretin (14 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pkm Pyruvate kinase isozymes M1/M2 (66 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pseudomonas aeruginosa (123386 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Klebsiella pneumoniae (43867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Acinetobacter baumannii (41033 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cryptococcus neoformans (21258 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Candida albicans (78123 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Luciferin 4-monooxygenase (66902 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PYK Pyruvate kinase (6726 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ddn Putative uncharacterized protein (49 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
fba Putative fructose-1,6-bisphosphate aldolase (15559 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504750534
分子类型 小分子
IIUPAC Name 2-amino-5-oxo-7-propan-2-ylchromeno[2,3-b]pyridine-3-carboxylic acid
INCHI 1S/C16H14N2O4/c1-7(2)8-3-4-12-9(5-8)13(19)10-6-11(16(20)21)14(17)18-15(10)22-12/h3-7H,1-2H3,(H2,17,18)(H,20,21)
InChi Key SGRYPYWGNKJSDL-UHFFFAOYSA-N
Smiles CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N
Isomeric SMILES CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N
分子量 298.29
Reaxy-Rn 556384
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=556384&ln=

化学和物理性质

敏感性 对空气敏感
熔点 300 °C
分子量 298.290 g/mol
XLogP3 3.100
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 298.095 Da
单同位素质量Monoisotopic Mass 298.095 Da
拓扑极表面积Topological Polar Surface Area 103.000 Ų
重原子数Heavy Atom Count 22
形式电荷Formal Charge 0
复杂度Complexity 467.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

象形图 GHS07
信号词 警告
危险声明

H302: 吞食有害
预防措施声明

P264: 处理后要彻底洗手。

P270: 使用本产品时，请勿进食、饮水或吸烟。

P330: 漱口

P301+P312: 如误吞咽：如感觉不适，呼叫急救中心/医生。

P501: 将内容物/容器处理到。。。
WGK Germany 3
Merck Index 490

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！

找到8个结果

批号(Lot Number) 证书类型 货号
I2424165 分析证书 A136009
I2424174 分析证书 A136009
I2424175 分析证书 A136009
C2306574 分析证书 A136009
C2306575 分析证书 A136009
D2110255 分析证书 A136009
D2110232 分析证书 A136009
D2110254 分析证书 A136009

可替换产品

  1. 氨来呫诺
    氨来呫诺

    ¥164.72

引用文献

1. Bell J.  (2005)  Amlexanox for the treatment of recurrent aphthous ulcers..  Clin Drug Investig,  25  (9): (555-66).  [PMID:17532700]
2. Spina D.  (2008)  PDE4 inhibitors: current status..  Br J Pharmacol,  155  (3): (308-15).  [PMID:18660825]
3. Elad S, Epstein JB, von Bültzingslöwen I, Drucker S, Tzach R, Yarom N.  (2011)  Topical immunomodulators for management of oral mucosal conditions, a systematic review; Part II: miscellaneous agents..  Expert Opin Emerg Drugs,  16  (1): (183-202).  [PMID:21244328]
4. Reilly SM, Chiang SH, Decker SJ, Chang L, Uhm M, Larsen MJ, Rubin JR, Mowers J, White NM, Hochberg I et al..  (2013)  An inhibitor of the protein kinases TBK1 and IKK-ɛ improves obesity-related metabolic dysfunctions in mice..  Nat Med,  19  (3): (313-21).  [PMID:23396211]
5. Makino H, Saijo T, Ashida Y, Kuriki H, Maki Y.  (1987)  Mechanism of action of an antiallergic agent, amlexanox (AA-673), in inhibiting histamine release from mast cells. Acceleration of cAMP generation and inhibition of phosphodiesterase..  Int Arch Allergy Appl Immunol,  82  (1): (66-71).  [PMID:2433225]
6. Mowers J, Uhm M, Reilly SM, Simon J, Leto D, Chiang SH, Chang L, Saltiel AR.  (2013)  Inflammation produces catecholamine resistance in obesity via activation of PDE3B by the protein kinases IKKε and TBK1..  Elife,  2  (e01119).  [PMID:24368730] [10.7554/eLife.01119]
7. Hansen IS, Krabbendam L, Bernink JH, Loayza-Puch F, Hoepel W, van Burgsteden JA, Kuijper EC, Buskens CJ, Bemelman WA, Zaat SAJ et al..  (2018)  FcαRI co-stimulation converts human intestinal CD103+dendritic cells into pro-inflammatory cells through glycolytic reprogramming..  Nat Commun,  9  (1): (863).  [PMID:29491406]
8. Adzika GK et al..  (2021)  Amlexanox and Forskolin Prevents Isoproterenol-Induced Cardiomyopathy by Subduing Cardiomyocyte Hypertrophy and Maladaptive Inflammatory Responses..  Front Cell Dev Biol,  9  (719351).  [PMID:34631707]
9. McCarthy GM et al..  (2018)  Chronic ethanol consumption: role of TLR3/TRIF-dependent signaling..  Addict Biol,  23  (3): (889-903).  [PMID:28840972]
10. Adzika GK et al..  (2021)  Isoproterenol-Induced Cardiomyopathy Recovery Intervention: Amlexanox and Forskolin Enhances the Resolution of Catecholamine Stress-Induced Maladaptive Myocardial Remodeling..  Front Cardiovasc Med,  8  (719805).  [PMID:34901202]
11. Huh JY et al..  (2020)  TANK-Binding Kinase 1 Regulates the Localization of Acyl-CoA Synthetase ACSL1 to Control Hepatic Fatty Acid Oxidation..  Cell Metab,  32  (6): (1012-1027.e7).  [PMID:33152322]
12. Sawaged S et al..  (2022)  TBK1 and GABARAP family members suppress Coxsackievirus B infection by limiting viral production and promoting autophagic degradation of viral extracellular vesicles..  PLoS Pathog,  18  (8): (e1010350).  [PMID:36044516]
13. Zhao P et al..  (2018)  TBK1 at the Crossroads of Inflammation and Energy Homeostasis in Adipose Tissue..  Cell,  172  (4): (731-743.e12).  [PMID:29425491]
14. Zhao P et al..  (2022)  The TBK1/IKKe inhibitor amlexanox improves dyslipidemia and prevents atherosclerosis..  JCI Insight,  7  (17): [PMID:35917178]
15. Eintracht J et al..  (2021)  Translational readthrough of ciliopathy genes BBS2 and ALMS1 restores protein, ciliogenesis and function in patient fibroblasts..  EBioMedicine,  70  (103515).  [PMID:34365092]

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