Home Neuronal Signaling Beta Amyloid inhibitor - Gamma-secretase inhibitor FPS-ZM1 For research use only.

FPS-ZM1

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.

FPS-ZM1 Chemical Structure

FPS-ZM1 Chemical Structure

CAS No. 945714-67-0

Purity & Quality Control

FPS-ZM1 Related Products

Signaling Pathway

Beta Amyloid Signaling Pathways

Beta Amyloid Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO Function assay Displacement of [I125]amyloid beta (1 to 40) from human RAGE domain V expressed in CHO cells, Ki=0.025μM 28482155
CHO Function assay Inhibition of HMGB1 binding to human RAGE domain V expressed in CHO cells, Ki=0.148μM 28482155
CHO Function assay Inhibition of S110B binding to human RAGE domain V expressed in CHO cells, Ki=0.23μM 28482155
Click to View More Cell Line Experimental Data

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
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence AGE-2 / AGEE-3 cathepsin B Caspase-1 29430285
In Vivo
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].
Animal Research Animal Models C57BL/6 mice
Dosages 1 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 327.85 Formula

C20H22ClNO
CAS No. 945714-67-0 SDF Download FPS-ZM1 SDF
Smiles C1CCC(CC1)N(CC2=CC=CC=C2)C(=O)C3=CC=C(C=C3)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (201.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 66 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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