AZ-3451

A PAR2 antagonist

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库存: 现货

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数量
5mg

￥887.00

710.00

- +
10mg

￥1525.00

1220.00

- +
25mg

￥3425.00

2740.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci20546
CAS: 2100284-59-9
别名: (S)-2-(6-溴苯并[D][1,3]二氧杂环戊烯-5-基)-N-(4-氰基苯基)-1-(1-环己基乙基)-1H-苯并[D]咪唑-5-甲酰胺
分子式: C30H27BrN4O3
分子量: 571.46
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

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/K_D

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)