Amlexanox

製品コードS3648 バッチS364805

印刷

化学情報

Synonyms

CHX-3673, Amoxanox, AA-673

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₆H₁₄N₂O₄

分子量

298.29

CAS No.

68302-57-8

Solubility (25°C)*

体外

DMSO

60 mg/mL (201.14 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and 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^[1].
in vivo	Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	3T3-L1 adipocytes
	濃度	12, 25, 50 μM
	反応時間	1 h
	実験の流れ	TBK1 phosphorylation (pTBK1) at Ser172 and IRF3 phosphorylation at Ser396 (pIRF3) in 3T3-L1 adipocytes treated with amlexanox or cayman and with or without poly I:C are examined.
動物実験	動物モデル	C57BL/6
	投薬量	25 or 100 mg per kg body weight
	投与方法	oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/23396211/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Development of a TBK1 and ALK dual inhibitor for alleviating depressive behavior via anti-inflammatory effects [ Biomed Pharmacother, 2025, 186:117991]	PubMed: 40117902
Development of translational read-through-inducing drugs as novel therapeutic options for patients with Fanconi anemia [ Cell Death Discov, 2025, 11(1):286]	PubMed: 40544182
Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis [ Sci Adv, 2025, 11(4):eadq2395]	PubMed: 39841821
Targeting TANK-binding kinase 1 attenuates painful diabetic neuropathy via inhibiting microglia pyroptosis [ Cell Commun Signal, 2024, 22(1):368]	PubMed: 39030571
Therapeutic modulation of ROCK overcomes metabolic adaptation of cancer cells to OXPHOS inhibition and drives synergistic anti-tumor activity [ bioRxiv, 2024, 2024.09.16.613317]	PubMed: 39345502
TRIM28 promotes the escape of gastric cancer cells from immune surveillance by increasing PD-L1 abundance [ Signal Transduct Target Ther, 2023, 8(1):246]	PubMed: 37357254
TRIM28 promotes the escape of gastric cancer cells from immune surveillance by increasing PD-L1 abundance [ Signal Transduct Target Ther, 2023, 8(1):246]	PubMed: 37357254
FACT subunit SUPT16H associates with BRD4 and contributes to silencing of interferon signaling [ Nucleic Acids Res, 2022, 50(15):8700-8718]	PubMed: 35904816
Mouse Ocilrp2/Clec2i negatively regulates LPS-mediated IL-6 production by blocking Dap12-Syk interaction in macrophage [ Front Immunol, 2022, 13:984520]	PubMed: 36300111
Host MOV10 is induced to restrict herpes simplex virus 1 lytic infection by promoting type I interferon response [ PLoS Pathog, 2022, 18(2):e1010301]	PubMed: 35157734

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。