Azeliragon (TTP488)

製品コードS6415 バッチS641502

印刷

化学情報

 Chemical Structure Synonyms PF-04494700 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C32H38ClN3O2

分子量 532.12 CAS No. 603148-36-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (187.92 mM)
Ethanol 100 mg/mL (187.92 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
6.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 120 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 Corn oil
6.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 120 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 Azeliragon (TTP488, PF-04494700) is an orally bioavailable small molecule that inhibits the receptor for advanced glycation endproducts (RAGE), which is an immunoglobulin-like cell surface receptor overexpressed in brain tissues of patients with AD.
in vivo

Preclinical studies in animal models of alzheimer disease (tgAPPSwedish/London) have shown azeliragon to decrease Aβ plaque deposition; reduce total Aβ brain concentration while increasing plasma Aβ levels; decrease sAPPβ while increasing sAPPα; reduce levels of inflammatory cytokines; and slow cognitive decline and improve cerebral blood flow[1].

プロトコル(参考用のみ)

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:

Macrophage RAGE activation is proinflammatory in NASH [ JCI Insight, 2024, e169138] PubMed: 38175729
Azeliragon inhibits PAK1 and enhances the therapeutic efficacy of AKT inhibitors in pancreatic cancer [ Eur J Pharmacol, 2023, 948:175703] PubMed: 37028543
Modulating the RAGE-Induced Inflammatory Response: Peptoids as RAGE Antagonists [ Chembiochem, 2023, 10.1002/cbic.202300503] PubMed: 37679300
The receptor for advanced glycation end products mediates dysfunction of airway epithelial barrier in a lipopolysaccharides-induced murine acute lung injury model [ Int Immunopharmacol, 2021, 93:107419] PubMed: 33548580
Tumor-derived HMGB1 induces CD62Ldim neutrophil polarization and promotes lung metastasis in triple-negative breast cancer [ Oncogenesis, 2020, 9(9):82] PubMed: 32943604
Carnosine Stimulates Macrophage-Mediated Clearance of Senescent Skin Cells Through Activation of the AKT2 Signaling Pathway by CD36 and RAGE [ Front Pharmacol, 2020, 11:593832] PubMed: 33390976

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。