A PAR2 antagonist
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AZ3451

Item No. 29671

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    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).1 It is selective for PAR2 over PAR4 and PAR1 (IC50s = <2.5, 380, and >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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cheng, R.K.Y., Fiez-Vandal, C., Schlenker, O., et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature 545(7652), 112-115 (2017).