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FPS-ZM1

Cat. No. M8968
FPS-ZM1 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 50  USD50 In stock
10mg USD 90  USD90 In stock
25mg USD 160  USD160 In stock
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Quality Control
Biological Activity

FPS-ZM1 is a high-affinity RAGE specific inhibitor with a Ki of 25 nM. 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. 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 (BBB) in vivo. FPS-ZM1 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.

Protocol
Cell Experiment
Cell lines CHO cells
Preparation 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 CCK-8 Assay Kit.
Concentrations 10 nM to 10 μM
Incubation time 72 h
Animal Experiment
Animal models C57BL/6 mice
Formulation PBS
Dosages 1 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 327.85
Formula C20H22ClNO
CAS Number 945714-67-0
Purity 99.76%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
References

[1] Hong Y, et al. Neurochem Res. Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus.

[2] Deane R, et al. J Clin Invest. A multimodal RAGE-specific inhibitor reduces amyloid β-mediated brain disorder in a mouse model of Alzheimer disease.

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  Catalog
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Keywords: FPS-ZM1 supplier, Amyloid, inhibitors

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