Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Target K_i: 25, 148, and 230 nM, respectively, against A&beta

Primary TargetRAGE

General description

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 (K_i = 25, 148, and 230 nM, respectively, against Aβ40, HMGB1, and S100B, binding to sRAGE). Blocks RAGE-mediated influx of Aβ40 and Aβ42 into the brain. Also shown to suppress Aβ-RAGE induced NF-κB activation and NF-κB-dependent transcription of β-secretase. Daily treatment of APP^sw/0 murine AD model (1 mg/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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Deane, R., et al. 2012. J. Clin. Invest.122, 1377.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)