AZ 3451 - ≥98%(HPLC), high purity , CAS No.2100284-59-9, Allosteric modulator of PAR2

Item Number
A286695
Grouped product items
SKUSizeAvailabilityPrice Qty
A286695-5mg
5mg
In stock
$75.90
A286695-10mg
10mg
In stock
$129.90
A286695-25mg
25mg
In stock
$293.90
A286695-50mg
50mg
In stock
$510.90
A286695-100mg
100mg
In stock
$891.90

Potent negative allosteric modulator of PAR2receptors

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent negative allosteric modulator of PAR2(IC50= 23 nM); binds to a remote allosteric site outside the helical bundle. Inhibits ERK phosphorylation in 1321N1 cells overexpressing wild-type human PAR2. Highly lipophilic.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric modulator of PAR2
Product Description

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.

Associated Targets(Human)

F2RL1 Tchem Proteinase-activated receptor 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
F2R Tclin Proteinase-activated receptor 1 (1799 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
F2RL3 Tchem Proteinase activated receptor 4 (1491 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
F2RL1 Tchem Proteinase-activated receptor 2 (703 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2-(6-bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]benzimidazole-5-carboxamide
INCHI InChI=1S/C30H27BrN4O3/c1-18(20-5-3-2-4-6-20)35-26-12-9-21(30(36)33-22-10-7-19(16-32)8-11-22)13-25(26)34-29(35)23-14-27-28(15-24(23)31)38-17-37-27/h7-15,18,20H,2-6,17H2,1H3,(H,33,36)/t18-/m0/s1
InChi Key FJAOGFGHTPYADT-SFHVURJKSA-N
Canonical SMILES CC(C1CCCCC1)N2C3=C(C=C(C=C3)C(=O)NC4=CC=C(C=C4)C#N)N=C2C5=CC6=C(C=C5Br)OCO6
Isomeric SMILES C[C@@H](C1CCCCC1)N2C3=C(C=C(C=C3)C(=O)NC4=CC=C(C=C4)C#N)N=C2C5=CC6=C(C=C5Br)OCO6
PubChem CID 126961335
MeSH Entry Terms 2-(6-bromobenzo(d)(1,3)dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1Hbenzo(d)imidazole-5-carboxamide;AZ3451
Molecular Weight 571.46

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
C2222194Certificate of AnalysisFeb 16, 2022 A286695
C2222204Certificate of AnalysisFeb 16, 2022 A286695
C2222213Certificate of AnalysisFeb 16, 2022 A286695
C2222270Certificate of AnalysisFeb 16, 2022 A286695

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 57.15, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 57.15, Max Conc. mM: 100

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