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 ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
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|---|
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Methyl tridecanoate inhibits β-amyloid aggregation. Methyl tridecanoate weakly inhibits acetylcholinesterase (AChE). |
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RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. |
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| β-Amyloid peptide(16-20)
β-Amyloid peptide(16-20) is a amino acid sequences (KLVFF) of Amyloid-β (Abeta). |
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