AZ-3451 |
| カタログ番号GC18152 |
AZ-3451 は、23 nM の IC50 を持つ強力なプロテアーゼ活性化受容体 2 (PAR2) アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2100284-59-9
Sample solution is provided at 25 µL, 10mM.
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AZ3451 is a protease-activated receptor-2 (PAR2) antagonist.
AZ3451 is highly lipophilic, which coincides with the hydrophobic nature of the binding pocket within the membrane. The interaction of AZ3451 with PAR2 is predominately hydrophobic in nature. AZ3451 binds to a remote allosteric site outside the helical bundle, which prevents structural rearrangements required for receptor activation and signaling.
IC50/KD
| IP-One(SLIGRL) | 23±1nM(n=72) |
| FLIPR(SLIGRL) | 5.4±1.1nM(n=11) |
| FLIPR(Trypsin) | 6.6±1.1μM(n=9) |
| Biacore(KD) | 13.5±3nM(n=3) |
| β-arrestin-2(PAR1) | >50μM(n=1) |
| β-arrestin-2(PAR2) | <2.5nM(n=1) |
| β-arrestin-2(PAR4) | 0.38μM(n=1) |
References:
1. Cheng RKY, et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017 May 4;545(7652):112-115.
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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