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 (Ki = 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 APPsw/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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
RAGE
Reversible: yes
Target Ki: 25, 148, and 230 nM, respectively, against A&beta
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Deane, R., et al. 2012. J. Clin. Invest.122, 1377.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 327.85. Empirical Formula: C20H22ClNO. Quality Level: 100. Assay: ≥. 98% (HPLC). form: semisolid, viscous liquid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: white to off-white. solubility: DMSO: 100 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: O: C(C1: CC: C(Cl)C: C1)N(CC2: CC: CC: C2)C3CCCCC3. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51292602
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 553030-25MG