| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| Other Sizes |
|
Amlexanox (Amoxanox; AA-673; CHX-3673), an effective and selective IKKε and TBK1 inhibitor, is used to treat recurrent aphthous ulcers (canker sores), as well as (in Japan) a number of inflammatory conditions. With an IC50 of roughly 1-2 μM, it inhibits the IKKε and TBK1 activity as determined by MBP phosphorylation. Amlexanox prevents mast cells, neutrophils, and mononuclear cells from producing and releasing inflammatory mediators like leukotrienes and histamine. Amlexanox also functions as a phosphodiesterase inhibitor and a leukotriene D4 antagonist. Amlexanox reduces ulcer pain and the amount of time it takes for ulcers to heal.
| Targets |
IKKε (IC50 = 1-2 μM); TBK1 (IC50 = 1-2 μM)
|
|---|---|
| ln Vitro |
Amlexanox has a dose-response relationship that inhibits IKK- and TBK1 activity by phosphorylating MBP, with an IC50 of roughly 1-2 μM. At roughly the same concentrations, amlexanox also inhibits the activity of TBK1, but it has no effect on IKK-α or IKK-β, and at these concentrations, it does not inhibit any other kinases from a large panel representing the majority of kinase families. Amlexanox competes with IKK-ɛ - or TBK1 for its substrate ATP, showing that it interacts with the enzymes in the ATP-binding site. Amlexanox increases the phosphorylation of TBK1 at Ser172 in 3T3-L1 adipocytes and inhibits the phosphorylation of interferon responsive factor-3 (IRF3), a presumed substrate of IKK-ɛ - and TBK1[1], when it is stimulated by polyinosinic:polycytidylic acid (poly I:C).
|
| ln Vivo |
Amlexanox therapy reduces steatosis, improves insulin sensitivity, and causes weight loss in obese mice through an increase in thermogenesis[1].
|
| Enzyme Assay |
The in vitro kinase assay is carried out by incubating purified kinase (IKK or TBK1) for 30 minutes at 30°C in the presence of 0.5 Ci µCi γ-[32P]--ATP and 1 g MBP per sample as a substrate in kinase buffer that contains 25 mM Tris (pH 7.5), 10 mM MgCl2, 1 mM DTT, and 10 µM ATP. When 4x sodium dodecyl sulfate (SDS) sample buffer is added, the kinase reaction is stopped by boiling for 5 minutes at 95°C. The Typhoon 9410 phosphorimager is used to conduct autoradiography analysis after supernatants have been resolved using SDS-polyacrylamide gel electrophoresis and transferred to nitrocellulose.
|
| Cell Assay |
The manufacturer's instructions are followed when using a Cell Counting Kit-8 to look at cell proliferation. BMMs are seeded in 96-well plates at a density of 5×103 cells per well. After 24 hours, cells are given treatments with varying doses of AmLexanox (0, 1.5, 3, 6, 12, 25 μM) every 2 days while being exposed to M-CSF (30 ng/mL) for a total of 7 days. The culture medium is changed to one containing 10% CCK-8 after 1, 3, 5, and 7 days, and cells are then incubated at 37°C for an additional 2 hours. On an ELX800 absorbance microplate reader, the absorbance is then measured at a wavelength of 450 nm.
|
| Animal Protocol |
In contrast to ND C57BL/6 controls, wildtype male C57BL/6 mice are fed a HFD starting at eight weeks of age for 12–24 weeks that contains 45% of their calories from fat. ω-3 fatty acids are included in the diets fed to C57BL/6 mice. Mice that have been on the HFD for 16 weeks receive a three-week course of rosiglitazone treatment by ingesting the medication. The average daily dose of rosiglitazone consumed by each mouse is 3.5 mg/kg. Every day oral gavage is used to administer AmLexanox. AmLexanox (25 mg or 100 mg per kg) administration for the prevention groups starts at eight weeks of age, concurrent with HFD feeding. After 12 weeks of HFD, the treatment groups start receiving 25 mg per kg of amLexanox at 20 weeks old. After eight weeks of amLexanox treatment, mice in the treatment group are switched from receiving amLexanox gavage to receiving a vehicle control to test the effects of amLexanox withdrawal. At ten weeks of age, control and ob/ob mice receive a standard chow diet along with 100 mg per kg of amLexanox or a vehicle control. The animals are kept in a facility that is specifically pathogen-free, has a 12-hour light/12-hour dark cycle, and they have unrestricted access to food and water.
|
| References |
| Molecular Formula |
C16H14N2O4
|
|---|---|
| Molecular Weight |
298.2934
|
| Exact Mass |
298.10
|
| Elemental Analysis |
C, 64.42; H, 4.73; N, 9.39; O, 21.45
|
| CAS # |
68302-57-8
|
| Related CAS # |
68302-57-8
|
| Appearance |
Solid powder
|
| SMILES |
CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N
|
| InChi Key |
SGRYPYWGNKJSDL-UHFFFAOYSA-N
|
| InChi Code |
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)
|
| Chemical Name |
2-amino-5-oxo-7-propan-2-ylchromeno[2,3-b]pyridine-3-carboxylic acid
|
| Synonyms |
CHX 3673 CHX-3673 CHX3673AA-673 AA673 AA 673 Amoxanox, Aphthasol.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 59~100 mg/mL (197.8~335.2 mM)
Ethanol: ~2 mg/mL(~6.7 mM) |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3524 mL | 16.7622 mL | 33.5244 mL | |
| 5 mM | 0.6705 mL | 3.3524 mL | 6.7049 mL | |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3524 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01083875 | Completed | Drug: amlexanox Drug: Vehicle rinse |
Oral Mucositis | Access Pharmaceuticals, Inc. | February 2000 | Phase 2 |
| NCT01975935 | Completed | Drug: Amlexanox Drug: Placebo |
Obesity Diabetes Mellitus Type 2 |
University of Michigan | January 2014 | Phase 3 |
|
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
