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Merck

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

Key Documents

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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).

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

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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:
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
Jianghong Zhong et al.
Communications biology, 4(1), 865-865 (2021-07-15)
A single-nucleotide polymorphism of neutrophil cytosolic factor 1 (Ncf1), leading to an impaired generation of reactive oxygen species (ROS), is a causative genetic factor for autoimmune disease. To study a possible tumor protection effect by the Ncf1 mutation in a
Rajkishor Nishad et al.
BMJ open diabetes research & care, 8(1) (2020-07-01)
Advanced glycation end-products (AGEs) are implicated in the pathogenesis of diabetic nephropathy (DN). Previous studies have shown that AGEs contribute to glomerulosclerosis and proteinuria. Podocytes, terminally differentiated epithelial cells of the glomerulus and the critical component of the glomerular filtration

Global Trade Item Number

SKUGTIN
553030-25MGCN04055977193466

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