2. Neuronal Signaling
  3. Amyloid-β
  4. FPS-ZM1

FPS-ZM1 is a high-affinity RAGE inhibitor with a Ki of 25 nM.

For research use only. We do not sell to patients.

FPS-ZM1 Chemical Structure

FPS-ZM1 Chemical Structure

CAS No. : 945714-67-0

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Customer Review

Based on 41 publication(s) in Google Scholar

FPS-ZM1 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE FPS-ZM1

WB
IF

    FPS-ZM1 purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2018 Oct;51(5):e12471  [Abstract]

    The effect of FPS-ZM1 treatment on osteogenic potential of adipose-derived stem cells (ASCs). FPS-ZM1 blocks RAGE in the FPS and advanced glycation end products (AGEs)+FPS-ZM1 groups.

    FPS-ZM1 purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2018 Nov 1;686:33-40.   [Abstract]

    Western Blot analyses show the protein expression of MCPIP1 after the treatment of PBS and LPS (with TAK-242, C29, FPS-ZM1).

    FPS-ZM1 purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2018 Nov 1;686:33-40.   [Abstract]

    Images show the expression of MCPIP1 after the treatment of of PBS and LPS (with TAK-242, C29, FPS-ZM1).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    FPS-ZM1 is a high-affinity RAGE inhibitor with a Ki of 25 nM.

    IC50 & Target

    Ki: 25 nM (RAGE)[1]
    In Vitro

    FPS-ZM1 inhibits Aβ/RAGE binding in CHO cells with approximately 2-fold greater affinity than its parent molecule, FPS2. FPS-ZM1 inhibits binding of other known RAGE ligands to sRAGE, including S100 calcium-binding protein B and amphoterin. FPS-ZM1 is more effective than FPS2 in reducing Aβ40-induced increases inBACE1 mRNA and protein levels and the generation of sAPPβ, an APP cleavage product of BACE1 indicative of BACE1 activity[1].

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

    FPS-ZM1 Related Antibodies
    In Vivo

    FPS-ZM1 is nontoxic to mice and readily crossed the blood-brain barrier. In aged APPsw/0 mice overexpressing human Aβ-precursor protein, a transgenic mouse model of AD with established Aβ pathology, FPS-ZM1 inhibits RAGE-mediated influx of circulating Aβ40 and Aβ42 into the brain. In brain, FPS-ZM1 binds exclusively to RAGE, which inhibits β-secretase activity and Aβ production and suppresses microglia activation and the neuro-inflammatory response[1]. FPS-ZM1 treatment reduces the level of Aβ1-40 and Aβ1-42 in AGEs Rats. It Inhibits AGEs-mediated increase of Aβ-metabolism-related proteins and downregulates AGEs-mediated increase of pro-inflammatory cytokines in the hippocampus. FPS-ZM1 up-Regulates anti-oxidant defense system and attenuated AGEs induced memory impairment in AGEs rats[2].

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

    327.85

    Formula

    C20H22ClNO
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC=C(C(N(C2CCCCC2)CC3=CC=CC=C3)=O)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (305.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (3.05 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0502 mL 15.2509 mL 30.5018 mL
    5 mM 0.6100 mL 3.0502 mL 6.1004 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.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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 (7.63 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 (7.63 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.
    Purity & Documentation

    Purity: 99.87%

    COA (250 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Human sRAGE is immobilized (10 μg/mL) overnight at 4°C in 96-well microtiter plates and blocked with 3% bovine serum albumin. 125I-labeled Aβ40, HMGB1, or S100B at 5 nM in the absence and presence of various concentrations of FPS2 or FPS-ZM1 (10 to 1,000 nM) is added to the wells containing immobilized sRAGE and incubated for 1 hour at room temperature in PBS. Wells are washed with cold PBS to remove unbound radiolabeled ligands, and the radioactivity is analyzed[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    To determine whether FPS2 and FPS-ZM1 are toxic to CHO cells, the cells are treated for 72 hours with different concentrations of inhibitors ranging from 10 nM to 10 μM. The cellular toxicity is determined using the WST-8 Assay Kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Rats: Starting from 1 week before intrahippocampal injection, FZM1 and AGEs+FZM1 rats are intraperitoneally injected with FPS-ZM1 (1 mg/kg/d at a volume of 2 mL) for 4 weeks; rats in the AGEs and the control groups are intraperitoneally injected with normal saline with the same volume for 4 weeks. Three weeks after AGEs intrahippocampal injection, the escape latency time of rats is assayed with Morris water maze test, and then all rats are sacrificed[2].

    Mice: FPS2 or FPS-ZM1 are administered i.v. (1 mg/kg) via the femoral vein and arterial blood samples (30 μL) collected at 1, 5, 10, 15, and 20 minutes via the cannulated femoral artery. Plasma is separated by centrifugation at 4°C and immediately stored at -80°C until analysis[1].

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

    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
    H2O / DMSO 1 mM 3.0502 mL 15.2509 mL 30.5018 mL 76.2544 mL
    DMSO 5 mM 0.6100 mL 3.0502 mL 6.1004 mL 15.2509 mL
    10 mM 0.3050 mL 1.5251 mL 3.0502 mL 7.6254 mL
    15 mM 0.2033 mL 1.0167 mL 2.0335 mL 5.0836 mL
    20 mM 0.1525 mL 0.7625 mL 1.5251 mL 3.8127 mL
    25 mM 0.1220 mL 0.6100 mL 1.2201 mL 3.0502 mL
    30 mM 0.1017 mL 0.5084 mL 1.0167 mL 2.5418 mL
    40 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9064 mL
    50 mM 0.0610 mL 0.3050 mL 0.6100 mL 1.5251 mL
    60 mM 0.0508 mL 0.2542 mL 0.5084 mL 1.2709 mL
    80 mM 0.0381 mL 0.1906 mL 0.3813 mL 0.9532 mL
    100 mM 0.0305 mL 0.1525 mL 0.3050 mL 0.7625 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    FPS-ZM1 Related Classifications

    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:

    FPS-ZM1945714-67-0Amyloid-ββ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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