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SML2050

AZ3451

≥98% (HPLC)

Synonym(s):

2-(6-Bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]-1H-benzimidazole-5-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C30H27BrN4O3
CAS Number:
Molecular Weight:
571.46
UNSPSC Code:
51111800
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

N#CC1=CC=C(NC(C2=CC=C(N([C@H](C3CCCCC3)C)C(C4=CC(OCO5)=C5C=C4Br)=N6)C6=C2)=O)C=C1

InChI key

FJAOGFGHTPYADT-SFHVURJKSA-N

Application

AZ3451 has been used as a protease-activated receptor 2 (PAR-2) antagonist to study the involvement of PAR-2 receptors in factor X activated (FXa)-induced upregulation of the cell adhesion molecules.[1]

Biochem/physiol Actions

AZ3451 exhibits anti-inflammatory function in vivo.[2] It can be used as a potential therapeutic for osteoarthritis (OA).[3]
AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2), a G protein-coupled receptor thought to be involved in inflammatory diseases, pain, allergic associated diseases (eosinophil migration, mast cells) and cancers. AZ3451 was found to bind to a remote allosteric site outside the helical bundle that is different from the site previously found on PAR1, and had an IC50 value of 23 nM. AZ3451 was able to completely inhibit ERK phosphorylation when added to 1321N1 cells overexpressing wild-type human PAR2.
Allosteric antagonist of protease-activated receptor 2 (PAR2)

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This Item
SML1184SML1515SML2825
assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear (warmed)

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

color

white to beige

color

white to beige

color

white to beige

color

white to beige


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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