AZ 3451

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Cat.No. 6806 - AZ 3451 | C30H27BrN4O3 | CAS No. 2100284-59-9
Description: Potent negative allosteric modulator of PAR2
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

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 57.15 100
ethanol 57.15 100

Preparing Stock Solutions

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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References

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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Citations for AZ 3451

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