For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Amlexanox (AA673; CHX3673) is a specific inhibitor of IKKε and TBK1; inhibition of IKKε and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1–2 μM.<br>IC50 value: 1-2 uM [1]<br>Target: TBK1/IKKε inhibitor<br>in vitro: Amlexanox blocked IKKε activity with a half maximal inhibitory concentration of approximately 1–2 μM. Amlexanox increased phosphorylation of TBK1 on Ser172 in 3T3-L1 adipocytes, and blocked polyinosinic:polycytidylic acid (poly I:C)-stimulated phosphorylation of interferon responsive factor-3 (IRF3), a presumed substrate of IKKε and TBK1[1].<br>in vivo: Fed C57Bl/6 mice a diet of 45% fat, and gavaged them daily with a vehicle control, 25 or 100 mg per kg amlexanox, while monitoring body weight, Treatment of animals with either dose of amlexanox prevented the weight gain produced by HFD; drug-treated mice maintained weights equivalent to those of vehicle-treated control diet mice throughout 12 weeks.treated DIO mice with 25 mg per kg amlexanox or vehicle control for eight weeks either before or after obesity was established, followed by assessment of metabolic parameters. Mice treated with amlexanox concurrently with HFD had improved glucose tolerance, with an approximate 30–40% reduction in the area under the curve for glucose [1]. After a 100mg dose of 5% amlexanox topical paste, applied directly to the lesion, the maximum serum concentration of the drug was 120 ng/mL, which was achieved 2.4 hours after application [2].</p>
| Catalog Number | I004569 |
| CAS Number | 68302-57-8 |
| Synonyms | AA 673; |
| Molecular Formula | C16H14N2O4 |
| Purity | ≥95% |
| Target | TBK1/IKKε inhibitor |
| Solubility | 100 mM in DMSO |
| Storage | -20°C |
| IC50 | 1-2 uM [1] |
| 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) |
| InChIKey | SGRYPYWGNKJSDL-UHFFFAOYSA-N |
| SMILES | CC(C)C1=CC=C2C(C(C(C=C(C(O)=O)C(N)=N3)=C3O2)=O)=C1 |
| Reference | </br>1:Effectiveness of Amlexanox and Adcortyl for the treatment of recurrent aphthous ulcers. Abbasi F, Raoof M, Khatami R, Shadman N, Borjian-Boroojeni F, Nazari F.J Clin Exp Dent. 2016 Oct 1;8(4):e368-e372. eCollection 2016 Oct. PMID: 27703603 Free PMC Article</br>2:Amlexanox Blocks the Interaction between S100A4 and Epidermal Growth Factor and Inhibits Cell Proliferation. Cho CC, Chou RH, Yu C.PLoS One. 2016 Aug 25;11(8):e0161663. doi: 10.1371/journal.pone.0161663. eCollection 2016. PMID: 27559743 Free PMC Article</br>3:Low-level laser therapy versus 5% amlexanox: a comparison of treatment effects in a cohort of minor aphthous ulcers patients-a commentary. Pentapati KC, Smriti K, Gadicherla S.Oral Surg Oral Med Oral Pathol Oral Radiol. 2016 Sep;122(3):373. doi: 10.1016/j.oooo.2016.02.021. Epub 2016 Jun 2. No abstract available. PMID: 27373585 </br>4:Low-level laser therapy versus 5% amlexanox: a comparison of treatment effects in a cohort of patients with minor aphthous ulcers. Jijin MJ, Rakaraddi M, Pai J, Jaishankar HP, Krupashankar R, Kavitha AP, Anjana R, Shobha R.Oral Surg Oral Med Oral Pathol Oral Radiol. 2016 Mar;121(3):269-73. doi: 10.1016/j.oooo.2015.11.021. Epub 2015 Dec 19. PMID: 26868469 </br>5:Amlexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Zhang Y, Guan H, Li J, Fang Z, Chen W, Li F.Sci Rep. 2015 Sep 4;5:13575. doi: 10.1038/srep13575. PMID: 26338477 Free PMC Article</br>6:Micelle-enhanced spectrofluorimetric determination of amlexanox in bioadhesive buccal tablets: application to content uniformity testing. Walash MI, Belal F, Tolba MM, Halawa MI.Luminescence. 2015 Sep;30(6):823-9. doi: 10.1002/bio.2828. Epub 2015 Jan 21. PMID: 25611457 </br>7:Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor. Homan KT, Wu E, Cannavo A, Koch WJ, Tesmer JJ.Molecules. 2014 Oct 22;19(10):16937-49. doi: 10.3390/molecules191016937. PMID: 25340299 Free PMC Article</br>8:Oral medicine: amlexanox. Ballal V, V J.Br Dent J. 2014 Sep;217(5):208. doi: 10.1038/sj.bdj.2014.770. No abstract available. PMID: 25213502 </br>9:Clinical study to know the efficacy of Amlexanox 5% with other topical Antiseptic, Analgesic and Anesthetic agents in treating minor RAS. Darshan DD, Kumar CN, Kumar AD, Manikantan NS, Balakrishnan D, Uthkal MP.J Int Oral Health. 2014 Feb;6(1):5-11. Epub 2014 Feb 26. PMID: 24653596 Free PMC Article</br>10:A clinical evaluation of 5% amlexanox oral paste in the treatment of minor recurrent aphthous ulcers and comparison with the placebo paste: a randomized, vehicle controlled, parallel, single center clinical trial. Bhat S, Sujatha D.Indian J Dent Res. 2013 Sep-Oct;24(5):593-8. doi: 10.4103/0970-9290.123382. PMID: 24355961 Free Article |
