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