FPS-ZM1

For research use only.

Catalog No.S8185

12 publications

FPS-ZM1 Chemical Structure

CAS No. 945714-67-0

FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE.

Selleck's FPS-ZM1 has been cited by 12 publications

3 Customer Reviews

  • FPS-ZM1 suppresses S100B promoted migration and invasion abilities. *P < 0.05, **P < 0.01 vs “CM” groups; &P < 0.05, &&P < 0.01 vs “S100B+FPS” groups.

    Biochem Biophys Res Commun, 2017, 495(1):78-85. FPS-ZM1 purchased from Selleck.

    (F) Representative immunohistochemical staining of β-catenin in the bronchial regions. Original magnification was 400× (n=6).

    Int Immunopharmacol, 2018, 59:187-196. FPS-ZM1 purchased from Selleck.

  • (F) Representative immunohistochemical staining of β-catenin in the bronchial regions. Original magnification was 400× (n = 6).(G) Western blot analysis of p-Lrp6, t-Lrp6, and RAGE in the whole lung. Representative immunoblots (bottom) and densitometric analyses (top) of protein levels normalized to β-actin levels were reported. (H) Western blot analysis of β-catenin target genes. Representative immunoblots (bottom) and densitometric analyses (top) of protein levels normalized to β-actin levels were reported. Data are expressed as mean ± SEMs (n = 6). *p < 0.05 compared with the AOO group; #p < 0.05 compared with the TDI group.

    International Immunopharmacology, 2018, 59:187-196. FPS-ZM1 purchased from Selleck.

Purity & Quality Control

Choose Selective Beta Amyloid Inhibitors

Biological Activity

Description FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE.
Targets
RAGE [1]
In vitro

FPS-ZM1 blocks Aβ binding to the V domain of RAGE and inhibited Aβ40- and Aβ42-induced cellular stress in RAGE-expressing cells in vitro. It blocks binding of other ligands to RAGE as well, such as S100B, AGE, and HMGB1, which have been suggested to contribute to RAGE-mediated long-term tissue damage in models of diabetes, immune/inflammatory disorders, and AD[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO MlP2SpVv[3Srb36gZZN{[Xl? NYLHUoV2TGm|cHzhZ4Vu\W62IH;mJHtKOTJ3XXHtfYxwcWRiYnX0ZUApOSC2bzC0NEkh\nKxbTDoeY1idiCUQVfFJIRwdWGrbjDWJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNuIFvpQVAvODJ3zszN MlrTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2OEKxOVUoRjJ6NEiyNVU2RC:jPh?=
CHO NXjYTWZITnWwY4Tpc44h[XO|YYm= M{C3OmlvcGmkaYTpc44hd2ZiSF3HRlEh[mmwZHnu[{B1dyCqdX3hckBTSUeHIHTvcYFqdiCYIHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEurPUCuNVQ5|ryP MlHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2OEKxOVUoRjJ6NEiyNVU2RC:jPh?=
CHO M17jd2Z2dmO2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKFNzMUDCJIJqdmSrbnegeI8hcHWvYX6gVmFITSCmb33hbY4hXiCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzMEBMcT1yLkKz{txO Moq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2OEKxOVUoRjJ6NEiyNVU2RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Immunofluorescence
AGE-2 / AGEE-3 ; 

PubMed: 29430285     


Effects of RAGE inhibitor on AGE-2 and AGE-3 uptake in J774.1 macrophages. The J774.1 macrophages were preincubated with different concentrations of FPS-ZM1 (RAGE inhibitor) at 37°C for 1 hr. Then, the cells were incubated with AGE-2 or AGE-3 (20 μg/ml) at 37°C for 30 min.

cathepsin B; 

PubMed: 31611559     


Effects of a RAGE inhibitor (FPS-ZM1) or the anti-HMGB1 antibody on the activation of cathepsin B were assessed.

Caspase-1; 

PubMed: 31611559     


Caspase-1 expression. Magnification: ×200, Scale bar = 100 μm.

29430285 31611559
In vivo FPS-ZM1 is nontoxic to mice and readily crossed the blood-brain barrier (BBB).It effectively controls progression of an Aβ-mediated brain disorder and the related neurovascular and cognitive dysfunction in 17-month-old APPsw/0 mice with fully developed Aβ and amyloid pathology by blocking RAGE actions at the BBB and in brain. Also, FPS-ZM1 blocks RAGE-dependent BACE1 expression and activity in brain of 17-month-old APPsw/0 mice[1].

Protocol

Cell Research:

[1]

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  • Cell lines: CHO cells
  • Concentrations: 10 nM to 10 μM
  • Incubation Time: 72 h
  • Method:

    CHO cells are treated for 72 hours with different concentrations of inhibitors ranging from 10 nM to 10 μM. The cellular toxicity was determined using the WST-8 Assay Kit.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: C57BL/6 mice
  • Dosages: 1 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 65 mg/mL (198.26 mM)
Ethanol 65 mg/mL (198.26 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
28mg/mL

* 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.

Chemical Information

Molecular Weight 327.85
Formula

C20H22ClNO

CAS No. 945714-67-0
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC(CC1)N(CC2=CC=CC=C2)C(=O)C3=CC=C(C=C3)Cl

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID