AZ 3451

Discontinued Product

AZ 3451 (Cat. No. 6806) has been withdrawn from sale for commercial reasons.
Description: Potent negative allosteric modulator of PAR2 receptors
Chemical Name: 2-(6-Bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]-1H-benzimidazole-5-carboxamide
Purity: ≥98% (HPLC)

Biological Activity for AZ 3451

AZ 3451 is a potent 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.

Compound Libraries for AZ 3451

AZ 3451 is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for AZ 3451

M. Wt 571.46
Formula C30H27BrN4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2100284-59-9
PubChem ID 126961335
Smiles C[C@H](N1C2=CC=C(C(NC3=CC=C(C#N)C=C3)=O)C=C2N=C1C4=C(C=C5OCOC5=C4)Br)C6CCCCC6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for AZ 3451

References are publications that support the biological activity of the product.

Cheng et al (2017) Structural insight into allosteric modulation of protease-activated receptor 2. Nature 545 112 PMID: 28445455

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Keywords: AZ 3451, AZ 3451 supplier, AZ3451, Potent, negative, allosteric, modulators, PAR2, antagonists, antagonism, F2R, like, trypsin, receptor, 1, protease-activated, Protease-Activated, Receptors, 6806, Tocris Bioscience

Citations for AZ 3451

Citations are publications that use Tocris products.

Currently there are no citations for AZ 3451.

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