553030

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).

• Synonym(s): RAGE Antagonist, FPS-ZM1, Receptor for AGE Antagonist, FPS-ZM1, N-Benzyl-4-chloro-N-cyclohexylbenzamide
• Empirical Formula (Hill Notation): C₂₀H₂₂ClNO
• Molecular Weight: 327.85
• MDL番号: MFCD22378757

Properties

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: semisolid; viscous liquid
• manufacturer/tradename: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white to off-white
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES string: O=C(C1=CC=C(Cl)C=C1)N(CC2=CC=CC=C2)C3CCCCC3

Description

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
RAGE

Reversible: yes

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

Safety Information

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable