AZ 3451

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (3)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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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View all Protease-Activated Receptor Modulators

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

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Currently there are no citations for AZ 3451. Do you know of a great paper that uses AZ 3451 from Tocris? Please let us know.

Reviews for AZ 3451

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Literature in this Area

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