A blood-brain-barrier-permeant, non-toxic, tertiary amide compound that acts as a high affinity, potent, multimodal blocker of RAGE (Receptor for Advanced Glycation End products) V domain-mediated ligand binding (Ki = 25, 148, and 230nM, respectively, against Ab40, HMGB1, and S100B, binding to sRAGE). Blocks RAGE-mediated influx of Ab40 and Ab42 into the brain. Also shown to suppress Ab-RAGE induced NF-kB activation and NF-kB-dependent transcription of b-secretase. Daily treatment of APPsw/0 murine AD model (1mg/kg/d via i.p.) is reported to greatly reduce Thioflavin S-positive amyloid plaques in cortex and hippocampus (by 70 to 80%) and restore congnitive performance to the level of non-AD mice.
Synonyms:N-Benzyl-4-chloro-N-cyclohexylbenzamide, Receptor for AGE Antagonist, FPS-ZM1
Formula:C₂₀H₂₂ClNO
Molecular Weight:327.9
Solubility:DMSO (100mg/ml)
Appearance:White to off-white semi-solid or viscous liquid
Purity:≥98% (HPLC)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
仕様
Size:25mg
Grade:Highly Purified
Purity:≥98% (HPLC)
Form:White to off-white semi-solid or viscous liquid