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. 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. FPS-ZM1 might be a novel therapeutic agent to treat AD patients.
Chemical Formula: C20H22ClNO
Exact Mass: 327.139
Molecular Weight: 327.852
Elemental Analysis: C, 73.27; H, 6.76; Cl, 10.81; N, 4.27; O, 4.88
InChi Code: 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
Appearance: White Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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. 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.
Hong Y, Shen C, Yin Q, Sun M, Ma Y, Liu X. Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus. Neurochem Res. 2016 May;41(5):1192-9. doi: 10.1007/s11064-015-1814-8. Epub 2016 Jan 6. PubMed PMID: 26738988.
Chen Y, Huang XJ, Yu N, Xie Y, Zhang K, Wen F, Liu H, Di Q. HMGB1 Contributes to the Expression of P-Glycoprotein in Mouse Epileptic Brain through Toll-Like Receptor 4 and Receptor for Advanced Glycation End Products. PLoS One. 2015 Oct 20;10(10):e0140918. doi: 10.1371/journal.pone.0140918. eCollection 2015. PubMed PMID: 26485677; PubMed Central PMCID: PMC4613137.
Li D, Lei C, Zhang S, Zhang S, Liu M, Wu B. Blockade of high mobility group box-1 signaling via the receptor for advanced glycation end-products ameliorates inflammatory damage after acute intracerebral hemorrhage. Neurosci Lett. 2015 Nov 16;609:109-19. doi: 10.1016/j.neulet.2015.10.035. Epub 2015 Oct 23. PubMed PMID: 26483322.
Good DW, George T, Watts BA 3rd. High-mobility group box 1 inhibits HCO(3)(-) absorption in medullary thick ascending limb through a basolateral receptor for advanced glycation end products pathway. Am J Physiol Renal Physiol. 2015 Oct 15;309(8):F720-30. doi: 10.1152/ajprenal.00227.2015. Epub 2015 Jul 15. PubMed PMID: 26180239; PubMed Central PMCID: PMC4609918.
Products are for research use only. Not for human use.
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