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FPS-ZM1 | RAGE receptor antagonist

CAS:
945714-67-0
Catalog Number:
10-4616
Activity:
RAGE receptor antagonist
Chemical Name:
4-Chloro-N-cyclohexyl-N-(phenylmethyl)benzamide
Molecular Weight:
327.85
Molecular Formula:
C20H22ClNO
Solubility:
Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

FPS-ZM1 (945714-67-0) is a high-affinity RAGE (Receptor for Advanced Glycation End products) receptor antagonist (IC50 = 0.6 μM). It lowers levels of Aβ via binding to the V domain of RAGE and can block multiple mechanisms of Aβ40- and Aβ42-induced cellular stress in RAGE-expressing brain endothelium, neurons and microglia in vitro and in vivo.1,2  Can cross the BBB.  In a rat model of intracerebral hemorrhage, FPS-ZM1 was able to attenuate blood-brain barrier and white matter fiber damage.3 FPS-ZM1 antagonism of RAGE was able to ameliorate inflammatory damage after acute intracerebral hemorrhage via downstream blockade of high mobility box-1(HMGB1) signaling.4  FPS-ZM1 has also been shown to impair breast cancer cell invasion and metastasis.5

References/Citations:

1) Deane et al. (2012), A multimodal RAGE-specific inhibitor reduces amyloid β-mediated brain disorder in a mouse model of Alzheimer disease; J. Clin. Invest. 122 1377
2) Hong et al. (2016), Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus ; Neurochem. Res. 41 1192
3) Yang et al. (2015), Receptor for advanced glycation end-product antagonist reduces blood-brain barrier damage after intracerebral hemorrhage; Stroke 46 1328
4) Li et al. (2015), Blockade of high mobility box-1 signaling via the receptor for advanced end-products ameliorates inflammatory damage after acute intracerebral hemorrhage; Neurosci. Lett. 609 109
5) Kwak et al. (2017), Targeting of RAGE-ligand signaling impairs breast cancer cell invasion and metastasis; Oncogene 36 155

FPS-ZM1 | RAGE receptor antagonist is also available in the Cellular Metabolism Library.
CAS:
945714-67-0
Catalog Number:
10-4616
Activity:
RAGE receptor antagonist
Chemical Name:
4-Chloro-N-cyclohexyl-N-(phenylmethyl)benzamide
Molecular Weight:
327.85
Molecular Formula:
C20H22ClNO
Solubility:
Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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