1. Neuronal Signaling
  2. Amyloid-β

FPS-ZM1 

Cat. No.: HY-19370 Purity: 99.31%
Handling Instructions

FPS-ZM1 is a high-affinity RAGE specific 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    FPS-ZM1 purchased from MCE. Usage Cited in: Brain Behav Immun. 2017 Jan;59:322-332.

    Pretreatment with TAK-242 restores the reduction of hippocampal MBP induced by ds-HMGB1. (A and B) MBP content is detected by Western blot analysis using antibodies against MBP. GAPDH is used to control the load quantity.

    FPS-ZM1 purchased from MCE. Usage Cited in: Cell Prolif. 2018 Jul 16:e12471.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    FPS-ZM1 is a high-affinity RAGE specific 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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.3050 mL 1.5251 mL 3.0502 mL
    Please refer to the solubility information to select the appropriate solvent.
    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
    Molecular Weight

    327.85

    Formula

    C₂₀H₂₂ClNO

    CAS No.

    945714-67-0

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    FPS-ZM1 is prepared in vehicle (normal saline)[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    FPS-ZM1
    Cat. No.:
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