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Amlexanox - ≥98.0%(HPLC), high purity , Phosphodiesterase 4 inhibitor, CAS No.68302-57-8, Phosphodiesterase 4 inhibitor

  • Moligand™
  • ≥98%(HPLC)
Item Number
A136009
Grouped product items
SKUSizeAvailabilityPrice Qty
A136009-250mg
250mg
In stock
$19.90
A136009-1g
1g
In stock
$49.90
A136009-5g
5g
In stock
$149.90

Selective TBK1 and IKKε inhibitor

Basic Description

Synonymsamlexanox|68302-57-8|Amoxanox|Aphthasol|2-Amino-7-isopropyl-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid|Amlenanox|Elics|AA-673|Amlexanoxo|Amlexanoxum|Amlexanoxum [Latin]|Amlexanoxo [Spanish]|CHX 3673|aphtheal|CHX-3673|AA 673|2-amino-5-oxo-7-(propan
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsSelective TBK1 and IKKε inhibitor (IC 50 = 1-2 μM). Shows antiallergic, antiobesogenic and anti-inflammatory effects in vivo. Orally active.
Storage TempStore at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionPhosphodiesterase 4 inhibitor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Product Properties

ALogP3.1

Associated Targets

CNR1 Tclin Cannabinoid receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD1 Tclin D(1A) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ERICH5 Tdark Glutamate-rich protein 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESR1 Tclin Estrogen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EHMT2 Tchem Histone-lysine N-methyltransferase EHMT2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NR3C1 Tclin Glucocorticoid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TTR Tclin Transthyretin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GAA Tclin Lysosomal alpha-glucosidase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TBXA2R Tclin Thromboxane A2 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MLNR Tchem Motilin receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 2-amino-5-oxo-7-propan-2-ylchromeno[2,3-b]pyridine-3-carboxylic acid
INCHI 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
Canonical 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
WGK Germany 3
PubChem CID 2161
Molecular Weight 298.29

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

5 results found

Lot NumberCertificate TypeDateItem
C2306574Certificate of AnalysisMar 15, 2023 A136009
C2306575Certificate of AnalysisMar 10, 2023 A136009
D2110232Certificate of AnalysisJan 16, 2023 A136009
D2110254Certificate of AnalysisJan 16, 2023 A136009
D2110255Certificate of AnalysisJan 16, 2023 A136009

Chemical and Physical Properties

Sensitivityair sensitive
Melt Point(°C)300 °C

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H302:Harmful if swallowed

Precautionary Statements

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

WGK Germany 3
Merck Index 490

Related Documents

References

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,  (3): (e01119).  [PMID:24368730]
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,  (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,  (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,  (719805).  [PMID:34901202]
11. 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]
12. 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]
13. 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]
14. 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]
15. Zhao P et al..  (2022)  The TBK1/IKKe inhibitor amlexanox improves dyslipidemia and prevents atherosclerosis..  JCI Insight,  (17):   [PMID:35917178]

Solution Calculators