AZ-3451 |
| Catalog No.GC18152 |
AZ-3451은 IC50이 23nM인 강력한 프로테아제 활성화 수용체-2(PAR2) 길항제입니다.
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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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