Name: Amlexanox
Brand: Selleck Chemicals
SKU: S3648
Rating: 5 (17 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.93%

99.93

Gerelateerde doelwitten	PD-1/PD-L1 CXCR STING AhR CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor
Overig Immunology & Inflammation related Inhibitoren	Cl-amidine Bestatin (Ubenimex) Bindarit (AF 2838) Tempol Tranilast Sinomenine GI254023X (GI4023) Geniposidic acid CORM-3 Oxymatrine

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
ARPE-19 cells	Function assay	1 μM		Inhibition of TBK1 by Amlx (1 µM) reduces HG-induced mitophagic flux
HCT-116	Function assay	100 μM	48 h	Amlexanox stimulates expression from a NMD reporter vector.
PC3	Function assay	20 nM, 100 nM, 1μM and 5 μM		leads to dosage-dependent downregulation of EMT-inducing transcriptional factors Zeb1 and N-cadherin, and upregulation of epithelial-specific protein E-cadherin
DU145	Function assay	20 nM, 100 nM, 1μM and 5 μM		leads to dosage-dependent downregulation of EMT-inducing transcriptional factors Zeb1 and N-cadherin, and upregulation of epithelial-specific protein E-cadherin
U87	Proliferation assay	0-300 μM	24, 48, 72 and 96 h	The IC50 values for 72 h of amlexanox treatment were approximately 140 μM in U87 cells.
U251	Proliferation assay	0-300 μM	24, 48, 72 and 96 h	The IC50 values for 72 h of amlexanox treatment were approximately 120 μM in U251 cells.
NIH 3T3 cells	Function assay	1 mM or 0.375 mM	24 h	Cells exhibited a dramatic change in their morphology that included a larger and more flattened phenotype and often displayed long processes that are stable for at least 10 days
HUVEC	Function assay	1 mM or 0.375 mM	24 h	modify cell morphology
Swiss 3T3	Function assay	1 mM	10-360 min	Amlexanox was able to stimulate the tyrosine phosphorylation of cortactin in a rapid and sustained manner.
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	298.29	Formule	C₁₆H₁₄N₂O₄	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	68302-57-8	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	CHX-3673, Amoxanox, AA-673			Smiles	CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 59 mg/mL (197.79 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

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In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.100mg/ml (7.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.100mg/ml (7.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	TBK1 IKK-ε
In vitro	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. This compound 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 this chemical is competitive for its substrate ATP, indicating that it interacts with the enzymes in the ATP-binding site. It 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.
In vivo	Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/23396211/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	IKKε / TBK1 / IKKβ MMP2 / MMP9 IKBKE / MST1 / MST2 / p-MST / LAST1 / LAST2 / p-YAP1 / YAP1 / Axl / c-Myc / Cyr61 p-p65 / p-IκBα / S100A13		23396211
Growth inhibition assay	Cell viability		29048430

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2018-11-07)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT01975935	COMPLETED	Diabetes Mellitus Type 2; Non-alcoholic Fatty Liver Disease; Obesity	University of Michigan	2014-01	PHASE2
NCT01842282	TERMINATED	Diabetes Mellitus Type 2; Non Alcoholic Fatty Liver Disease; Obesity	University of Michigan	2013-07-19	PHASE2
NCT01083875	COMPLETED	Oral Mucositis	Access Pharmaceuticals, Inc.	2000-02	PHASE2

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Amlexanox Immunology & Inflammation related Modulator

Molecuulgewicht: 298.29

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

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In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Amlexanox Immunology & Inflammation related Modulator

Molecuulgewicht: 298.29

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)