AZ-3451

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AZ-3451

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2100284-59-9

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

AZ-3451 是一种有效的蛋白酶激活受体 2 (PAR2) 拮抗剂，IC50 为 23 nM。

Cas No.

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

化学名

(S)-2-(6-bromobenzo[d][1,3]dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1H-benzo[d]imidazole-5-carboxamide

Canonical SMILES

BrC1=CC2=C(OCO2)C=C1C3=NC4=CC(C(NC5=CC=C(C#N)C=C5)=O)=CC=C4N3[C@@H](C)C6CCCCC6

分子式

C₃₀H₂₇BrN₄O₃

分子量

571.46

溶解度

Soluble in DMSO

储存条件

Store at -20℃

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

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)

References:
1. Cheng RKY, et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017 May 4;545(7652):112-115.