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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 |
| InChI Key | FJAOGFGHTPYADT-SFHVURJKSA-N |
| 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.
Solubility Data for AZ 3451
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.15 | 100 | |
| ethanol | 57.15 | 100 |
Preparing Stock Solutions for AZ 3451
The following data is based on the product molecular weight 571.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.75 mL | 8.75 mL | 17.5 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.5 mL |
| 10 mM | 0.17 mL | 0.87 mL | 1.75 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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Product Datasheets for AZ 3451
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
If you know of a relevant reference for AZ 3451, please let us know.
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Citations for AZ 3451
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