553030

FPS-ZM1

≥98% (HPLC), semisolid,viscous liquid, RAGE antagonist, Calbiochem^®

• Synonyme(s) : RAGE Antagonist, FPS-ZM1, Receptor for AGE Antagonist, FPS-ZM1, N-Benzyl-4-chloro-N-cyclohexylbenzamide
• Formule empirique (notation de Hill) : C₂₀H₂₂ClNO
• Numéro CAS: 945714-67-0
• Poids moléculaire : 327.85
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD22378757
• Assay: ≥98% (HPLC)
• Form: semisolid, viscous liquid
• Storage condition: OK to freeze, protect from light

Propriétés

• Nom du produit: RAGE Antagonist, FPS-ZM1, RAGE Antagonist, FPS-ZM1, is a blood-brain-barrier permeant blocker of RAGE V domain-mediated ligand binding (K_i = 25, 148, & 230 nM, respectively, against Aβ40, HMGB1 & S100B, binding to sRAGE).
• Quality Segment: 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
• InChI: 1S/C20H22ClNO/c21-18-13-11-17(12-14-18)20(23)22(19-9-5-2-6-10-19)15-16-7-3-1-4-8-16/h1,3-4,7-8,11-14,19H,2,5-6,9-10,15H2
• InChI key: XDFKWGIBQMHSOH-UHFFFAOYSA-N

Description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
RAGE

Reversible: yes

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

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• Que se passe-t-il ?: WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable