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
• CAS Number: 945714-67-0
• Poids moléculaire : 327.85
• Numéro MDL: MFCD22378757
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Product Name: 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).
• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: semisolid; viscous liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white to off-white
• Solubilité: DMSO: 100 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: 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
• Clé InChI: XDFKWGIBQMHSOH-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
RAGE

Reversible: yes

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable