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FPS-ZM1 is a high-affinity, RAGE-specific inhibitor that obstructs Aβ binding to the V domain of RAGE.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $43 | In Stock | |
10 mg | $52 | In Stock | |
25 mg | $93 | In Stock | |
50 mg | $150 | In Stock | |
100 mg | $231 | In Stock | |
200 mg | $369 | In Stock | |
500 mg | $622 | In Stock | |
1 mL x 10 mM (in DMSO) | $48 | In Stock |
Description | FPS-ZM1 is a high-affinity, RAGE-specific inhibitor that obstructs Aβ binding to the V domain of RAGE. |
Targets&IC50 | RAGE:25 nM. (Ki) |
In vitro | 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. It blocks binding of other ligands to RAGE as well, such as S100B, AGE, and HMGB1, which have been suggested to contribute to RAGE-mediated long-term tissue damage in models of diabetes, immune/inflammatory disorders, and AD[1]. |
In vivo | FPS-ZM1 is nontoxic to mice and readily crossed the blood-brain barrier (BBB).It 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. Also, FPS-ZM1 blocks RAGE-dependent BACE1 expression and activity in brain of 17-month-old APPsw/0 mice[1]. |
Kinase Assay | Human sRAGE is immobilized (10 μg/mL) overnight at 4°C in 96-well microtiter plates and blocked with 3% bovine serum albumin. 125I-labeled Aβ40, HMGB1, or S100B at 5 nM in the absence and presence of various concentrations of FPS2 or FPS-ZM1 (10 to 1,000 nM) is added to the wells containing immobilized sRAGE and incubated for 1 hour at room temperature in PBS. Wells are washed with cold PBS to remove unbound radiolabeled ligands, and the radioactivity is analyzed[1]. |
Cell Research | 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 WST-8 Assay Kit. (Only for Reference) |
Molecular Weight | 327.85 |
Formula | C20H22ClNO |
Cas No. | 945714-67-0 |
Smiles | Clc1ccc(cc1)C(=O)N(Cc1ccccc1)C1CCCCC1 |
Relative Density. | 1.18 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 16.67 mg/mL (50.84 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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