AZ3451

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). It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a beta-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.Formal Name: 2-(6-bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]-1H-benzimidazole-5-carboxamide. CAS Number: 2100284-59-9. Molecular Formula: C30H27BrN4O3. Formula Weight: 571.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 232, 298 nm. SMILES: O=C(C1=CC(N=C(C2=C(Br)C=C(OCO3)C3=C2)N4[C@H](C5CCCCC5)C)=C4C=C1)NC6=CC=C(C#N)C=C6. InChi Code: 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.