An allosteric antagonist of PAR2; inhibits SLIGRL-induced calcium mobilization by wild-type and 10 mutant forms of PAR2 in a FLIPR assay (IC50s = 23 and 12-780 nM

AZ3451 – 5 mg

Brand:
Cayman
CAS:
2100284-59-9
Storage:
-20
UN-No:
Non-Hazardous - /

AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.  

 

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SKU: 29671 - 5 mg Category:

Description

An allosteric antagonist of PAR2; inhibits SLIGRL-induced calcium mobilization by wild-type and 10 mutant forms of PAR2 in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively); selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay); inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells at 10 µM

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

Synonyms: 

Molecular weight: 571.5

CAS: 2100284-59-9

Purity: ≥98%

Formulation: A solid

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