945714-67-0 Usage
Uses
Used in Pharmaceutical Industry:
N-benzyl-4-chloro-N-cyclohexylbenzaMide is used as a RAGE receptor antagonist for lowering levels of Aβ and blocking multiple mechanisms of Aβ40and Aβ42-induced cellular stress in RAGE-expressing brain endothelium, neurons, and microglia. It can cross the blood-brain barrier and has been shown to attenuate blood-brain barrier and white matter fiber damage in a rat model of intracerebral hemorrhage.
Used in Oncology:
N-benzyl-4-chloro-N-cyclohexylbenzaMide is used as an inhibitor of breast cancer cell invasion and metastasis. It has been shown to impair breast cancer cell invasion and metastasis by antagonizing RAGE.
in vitro
fps-zm1 was identified as a high-affinity inhibitor of the receptor for advanced glycation end products. fps-zm1 could block the binding of amyloid β (aβ) protein to rage and inhibit aβ40- and aβ42-induced cellular stress in rage-expressing cells [1].
in vivo
animal study found that fps-zm1 was nontoxic to mice and readily crossed the blood-brain barrier (bbb). in aged appsw/0 mice overexpressing human aβ-precursor protein, fps-zm1 could inhibit rage-mediated influx of circulating aβ40 and aβ42 into the brain. fps-zm1 bound exclusively to rage in brain, which inhibited β-secretase activity and aβ production and suppressed microglia activation and the neuroinflammatory response. moreover, the blockade of rage actions at the bbb and in the brain could reduce aβ40 and aβ42 levels in brain in aged appsw/0 mice [1].
References
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
Check Digit Verification of cas no
The CAS Registry Mumber 945714-67-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,4,5,7,1 and 4 respectively; the second part has 2 digits, 6 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 945714-67:
(8*9)+(7*4)+(6*5)+(5*7)+(4*1)+(3*4)+(2*6)+(1*7)=200
200 % 10 = 0
So 945714-67-0 is a valid CAS Registry Number.
945714-67-0Relevant articles and documents
Structure-activity relationships of small molecule inhibitors of RAGE-Aβ binding
Ross, Nathan T.,Deane, Rashid,Perry, Sheldon,Miller, Benjamin L.
, p. 7653 - 7658 (2013/08/23)
The Receptor for Advanced Glycation Endproducts ('RAGE') mediates transport of amyloid-β peptide (Aβ) into the brain, and is therefore an important target for the development of therapeutic agents for Alzheimer's disease. We describe structure-activity relationships for inhibition of RAGE-Aβ binding, derived from the analysis of a library of tertiary amides.