FPS-ZM1

• CAT Number: I005629
• CAS Number: 945714-67-0
• Molecular Formula: C₂₀H₂₂ClNO
• Molecular Weight: 327.85
• Purity: ≥95%
• Synonyms: 4-chloro-N-cyclohexyl-N-(phenylmethyl)-benzamide
• Target: Amyloid-β
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 25 ± 5 nM (Ki)
• InChI: InChI=1S/C20H22ClNO/c21-18-13-11-17(12-14-18)20(23)22(19-9-5-2-6-10-19)15-16-7-3-1-4-8-16/h1,3-4,7-8,11-14,19H,2,5-6,9-10,15H2
• InChIKey: XDFKWGIBQMHSOH-UHFFFAOYSA-N
• SMILES: C1CCC(CC1)N(CC2=CC=CC=C2)C(=O)C3=CC=C(C=C3)Cl

FPS-ZM1(cas# 945714-67-0) is a high-affinity RAGE-specific inhibitor that blocks Aβ binding to the V domain of RAGE with Ki of 25 ± 5 nM in RAGE-transfected CHO cells.

Reference

1:Neurochem Res. 2016 May;41(5):1192-9. doi: 10.1007/s11064-015-1814-8. Epub 2016 Jan 6. Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus.Hong Y,Shen C,Yin Q,Sun M,Ma Y,Liu X, PMID: 26738988 DOI: 10.1007/s11064-015-1814-8
Abstract: An increased level of advanced glycation end products (AGEs) is observed in brains of patients with Alzheimer/’s disease (AD). AGEs and receptor for AGEs (RAGE) play important roles in the pathogenesis of AD. FPS-ZM1 is a high-affinity RAGE-specific blocker that inhibits amyloid-β binding to RAGE, neurological damage and inflammation in the APP(sw/0) transgenic mouse model of AD. FPS-ZM1 is not toxic to mice and can easily cross the blood-brain barrier. In this study, an AGEs-RAGE-activated rat model were established by intrahippocampal injection of AGEs, then these rats were treated with intraperitoneal administration of FPS-ZM1 and the possible neuroprotective effects were investigated. We found that AGEs administration induced an-regulation of Abeta production, inflammation, and oxidative stress, and an increased escape latency of rats in the Morris water maze test, all of these are significantly reduced by FPS-ZM1 treatment. Our results suggest that the AGEs-RAGE pathway is responsible for cognitive deficits, and therefore may be a potential treatment target. FPS-ZM1 might be a novel therapeutic agent to treat AD patients.