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553030

FPS-ZM1

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

Synonym(s):

RAGE Antagonist, FPS-ZM1, Receptor for AGE Antagonist, FPS-ZM1, N-Benzyl-4-chloro-N-cyclohexylbenzamide

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About This Item

Empirical Formula (Hill Notation):
C20H22ClNO
CAS Number:
945714-67-0
Molecular Weight:
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
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Product Name

RAGE Antagonist, FPS-ZM1, RAGE Antagonist, FPS-ZM1, is a blood-brain-barrier permeant blocker of RAGE V domain-mediated ligand binding (Ki = 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

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

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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