2. Neuronal Signaling
  3. Amyloid-β
  4. Azeliragon

Azeliragon  (Synonyms: TTP488; PF-04494700)

製品番号: HY-50682 純度: 99.75%
COA 取扱説明書 Technical Support

Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 603148-36-3

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 70 在庫あり
Solution
10 mM * 1 mL in DMSO USD 70 在庫あり
Solid
5 mg $60 在庫あり
10 mg $100 在庫あり
25 mg $180 在庫あり
50 mg $320 在庫あり
100 mg $600 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Other Forms of Azeliragon:

Azeliragon 関連抗体

Top Publications Citing Use of Products

    Azeliragon purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Apr:139:156541.  [Abstract]

    Azeliragon (5 μM; 6 h) in neutrophils significantly restrained HMGB1-driven neutrophil migration.

    Azeliragon purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Apr:139:156541.  [Abstract]

    Azeliragon (5 μM; 6 h) in neutrophils, representative immunofluorescence micrographs of NETs generation.

    Azeliragon purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Apr:139:156541.  [Abstract]

    Azeliragon (5 μM; 6 h) in neutrophils decreased the protein expression by MPO, PAD4 and CitH3 detected by western blot.

    Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59.  [Abstract]

    Azeliragon (TTP488; 1 mg/kg; IP; twice per week for 40 days) in 8-week-old female NSG mice showed anti-tumor activity.

    Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59.  [Abstract]

    Azeliragon (TTP488; 1 mg/kg; IP; twice per week for 40 days) in 8-week-old female NSG mice showed no antiproliferative effect in vivo. Immunohistochemical analysis of 4175/NSG tumors for proliferation (Ki67).

    Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59.  [Abstract]

    Azeliragon (TTP488; 1 mg/kg; IP; twice per week for 40 days) in 8-week-old female NSG mice showed reduced lung metastasis, with TTP488 affecting metastasis more potently at this dose. Immunohistochemical analysis of human CK7 to assess for metastasis in 4175/NSG mouse lung tissue.

    Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59.  [Abstract]

    4T-1 cells were tail-vein injected into BALBc mice, and mice were treated IP twice per week with 1 mg/kg Azeliragon (TTP488) or FPS-ZM1 (or vehicle (DMSO) control). Representative IVIS images at day 13 are shown from n = 11 per group. Mice treated with either TTP488 or FPS-ZM1 had significantly reduced tumor burden (p = <0.05) in the lungs at day 13 compared to the vehicle controltreated mice.

    Azeliragon purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2023 May 4;25(5):886-898.  [Abstract]

    Azeliragon (TTP488; 3 mg/kg/days; given four days after tumor implantation for a two-week period) improved the survival of ic GL261-bearing mice.

    Azeliragon purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2023 May 4;25(5):886-898.  [Abstract]

    Azeliragon (TTP488;500 ng/mL; 2, 4, 6 days) did not affect the growth of primary human malignant glioma cell lines in vitro.

    • 生物活性

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    製品説明

    Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression with mild Alzheimer’s disease (AD)[1]. Azeliragon also can cross the blood-brain barrier (BBB)[2].

    Cellular Effect
    Cell Line Type Value Description References
    SUM149PT IC50
    5.292 μM
    Compound: Azeliragon
    Cytotoxicity against human triple negative SUM149PT cells assessed as cell viability measured by MTS assay
    Cytotoxicity against human triple negative SUM149PT cells assessed as cell viability measured by MTS assay
    		[PMID: 34763082]
    体外実験

    Azeliragon (4 nM; 16 hours; T cells) treatment inhibits of wild type mice (WT) but not the deletion of the receptor (RAGE-/- mice) T cells and significant reduction in the production of IFN-γ[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Azeliragon 関連抗体

    Cell Viability Assay[3]

    Cell Line: Purified T cells from RAGE-/- or WT B6 mice.
    Concentration: 4 nM
    Incubation Time: 16 hours
    Result: Inhibited of WT but not RAGE-/- T cells, and significantly reduced the level of IFN-γ.
    体内実験

    Azeliragon (100 mcg/d; intraperitoneal injection; every day) treatment reduces syngeneic islet graft and islet allograft in NOD and B6 mice (Islets were isolated from young prediabetic NOD/LtJ mice and transplanted into NOD mice with spontaneous diabetes; islets were isolated from WT BALB/c mice and transplanted into B6 mice with diabetes)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Prediabetic NOD/LtJ (6-7 week old) mice, NOD mice with spontaneous diabetes, WT BALB/c mice (8-10 week old) and B6 mice with diabetes [3].
    Dosage: 100 mcg/d
    Administration: Intraperitoneal injection; every day
    Result: Prolonged islet auto and allograft survival.
    臨床実験
    分子量

    532.12

    分子式

    C32H38ClN3O2
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    ClC1=CC=C(C=C1)OC2=CC=C(C=C2)N3C(CCCC)=NC(C(C=C4)=CC=C4OCCCN(CC)CC)=C3
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (93.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8793 mL 9.3964 mL 18.7928 mL
    5 mM 0.3759 mL 1.8793 mL 3.7586 mL
    10 mM 0.1879 mL 0.9396 mL 1.8793 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.75%

    COA (247 KB) HNMR (413 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8793 mL 9.3964 mL 18.7928 mL 46.9819 mL
    5 mM 0.3759 mL 1.8793 mL 3.7586 mL 9.3964 mL
    10 mM 0.1879 mL 0.9396 mL 1.8793 mL 4.6982 mL
    15 mM 0.1253 mL 0.6264 mL 1.2529 mL 3.1321 mL
    20 mM 0.0940 mL 0.4698 mL 0.9396 mL 2.3491 mL
    25 mM 0.0752 mL 0.3759 mL 0.7517 mL 1.8793 mL
    30 mM 0.0626 mL 0.3132 mL 0.6264 mL 1.5661 mL
    40 mM 0.0470 mL 0.2349 mL 0.4698 mL 1.1745 mL
    50 mM 0.0376 mL 0.1879 mL 0.3759 mL 0.9396 mL
    60 mM 0.0313 mL 0.1566 mL 0.3132 mL 0.7830 mL
    80 mM 0.0235 mL 0.1175 mL 0.2349 mL 0.5873 mL
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    Azeliragon Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Azeliragon603148-36-3TTP488 PF-04494700TTP 488TTP-488PF04494700PF 04494700PF-04494700Amyloid-ββ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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    製品名:
    Azeliragon
    製品番号:
    HY-50682
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