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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.
| 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. |
| Molecular Weight | 327.85 |
| Formula | C20H22ClNO |
| CAS Number | 945714-67-0 |
| Solubility (25°C) | DMSO ≥ 33 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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