FPS-ZM1

Catalog No.S8185 Batch:S818501

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Technical Data

Formula

C20H22ClNO
Molecular Weight 327.85 CAS No. 945714-67-0
Solubility (25°C)* In vitro DMSO 65 mg/mL (198.26 mM)
Ethanol 65 mg/mL (198.26 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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].
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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    C57BL/6 mice

  • Dosages

    1 mg/kg

  • Administration

    i.v.

Customer Product Validation

, , Biochem Biophys Res Commun, 2017, 495(1):78-85

Data from [Data independently produced by , , Int Immunopharmacol, 2018, 59:187-196]

Data from [Data independently produced by , , International Immunopharmacology, 2018, 59:187-196]

Selleck's FPS-ZM1 has been cited by 32 publications

The critical role of RAGE in severe influenza infection: A target for control of inflammatory response in the disease [ Clin Immunol, 2024, 262:110178] PubMed: 38460892
Circulating extracellular vesicles from patients with traumatic brain injury induce cerebrovascular endothelial dysfunction [ Pharmacol Res, 2023, 192:106791] PubMed: 37156450
The TRIM21-FOXD1-BCL-2 axis underlies hyperglycaemic cell death and diabetic tissue damage [ Cell Death Dis, 2023, 14(12):825] PubMed: 38092733
RAGE inhibition blunts insulin-induced oncogenic signals in breast cancer [ Breast Cancer Res, 2023, 25(1):84] PubMed: 37461077
RAGE inhibition blunts insulin-induced oncogenic signals in breast cancer [ Breast Cancer Res, 2023, 25(1):84] PubMed: 37461077
Effects of HMGB1/RAGE/cathespin B inhibitors on alleviating hippocampal injury by regulating microglial pyroptosis and caspase activation in neonatal hypoxic-ischemic brain damage [ J Neurochem, 2023, 167(3):410-426] PubMed: 37753942
Proinflammatory S100A9 Stimulates TLR4/NF-κB Signaling Pathways Causing Enhanced Phagocytic Capacity of Microglial Cells [ Immunol Lett, 2023, 255:54-61] PubMed: 36870421
Stratification of radiosensitive brain metastases based on an actionable S100A9/RAGE resistance mechanism [ Nat Med, 2022, 28(4):752-765] PubMed: 35411077
S100A9-CXCL12 activation in BRCA1-mutant breast cancer promotes an immunosuppressive microenvironment associated with resistance to immunotherapy [ Nat Commun, 2022, 13(1):1481] PubMed: 35304461
Elevated neutrophil extracellular traps by HBV-mediated S100A9-TLR4/RAGE-ROS cascade facilitate the growth and metastasis of hepatocellular carcinoma [ Cancer Commun (Lond), 2022, 10.1002/cac2.12388] PubMed: 36346061

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.