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Merck

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

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A propos de cet article

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
Quality level:
100
Storage condition:
OK to freeze
protect from light

Principaux documents

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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 (Ki = 25, 148, & 230 nM, respectively, against Aβ40, HMGB1 & S100B, binding to sRAGE).

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

SMILES string

O=C(C1=CC=C(Cl)C=C1)N(CC2=CC=CC=C2)C3CCCCC3

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

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

Cell permeable: yes
Primary Target
RAGE
Reversible: yes
Target Ki: 25, 148, and 230 nM, respectively, against A&beta

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

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.

Legal Information

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificats d'analyse (COA)

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Muskan Rajkumar Thakur et al.
Journal of biochemical and molecular toxicology, 38(3), e23664-e23664 (2024-02-19)
The present work elucidates the role of colchicine (COL) on albumin glycation and cellular oxidative stress in diabetic cardiomyopathy (DCM). Human serum albumin (HSA) was glycated with methylglyoxal in the presence of COL (2.5, 3.75, and 5 µM), whereas positive and negative
Vijayasree V Giridharan et al.
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, 18(1), 640-653 (2020-09-05)
Pneumococcal meningitis is a life-threatening infection of the central nervous system (CNS), and half of the survivors of meningitis suffer from neurological sequelae. We hypothesized that pneumococcal meningitis causes CNS inflammation via the disruption of the blood-brain barrier (BBB) and
Han-Kyul Nam et al.
Biological & pharmaceutical bulletin, 44(11), 1697-1706 (2021-11-02)
Advanced glycation end products (AGEs) are the products formed through a non-enzymatic reaction of reducing sugars with proteins or lipids. There is a potential for toxicity in the case of AGEs produced through glycation with dicarbonyl compounds including methylglyoxal, glyoxal
Yidi Wu et al.
American journal of physiology. Lung cellular and molecular physiology, 319(1), L185-L195 (2020-05-21)
S100A4 is a low-molecular-mass (12 kDa) EF-hand Ca2+-binding S100 protein that is expressed in a broad range of normal tissue and cell types. S100A4 can be secreted from some cells to act in an autocrine or paracrine fashion on target
Chao Song et al.
Brain sciences, 12(5) (2022-05-29)
(1) Background: Chemotherapy-induced cognitive impairment (CICI) is often observed in cancer patients and impairs their life quality. Grape-seed-orientated procyanidin has been shown to have anti-inflammatory and neuroprotective effects, yet its effects in preventing CICI have not been investigated. (2) Method:
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