AZ3451

产品说明书

Print
Chemical Structure| 2100284-59-9 同义名 : -
CAS号 : 2100284-59-9
货号 : A595701
分子式 : C30H27BrN4O3
纯度 : 99%+
分子量 : 571.464
MDL号 : MFCD31728469
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(183.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Protease-activated receptors are a family of G-protein-coupled receptors implicated in inflammation, cell differentiation and proliferation. AZ3451 is an inhibitor of wild-type protease-activated receptor 2 (PAR2) with an IC50 value of 23 nM. AZ3451 also showed inhibitory effect on PAR2s with a single-point mutation on N222Q, H227A, H227Q, D228A, D228N, H135Y, I327L, G157M, Y210L, and F154A with IC50 values of 12, 12, 25, 23, 4.3, 20, 32, 780, 570 and 370 nM, respectively. In 1321N1 cells overexpressing wild-type human PAR2, stimulation of 1321N1 with SLIGRL led to the phosphorylation of extracellular signal-regulated kinase (ERK), whereas the induction of ERK phosphorylation was completely inhibited by AZ3451 at the concentration of 10 μM. The IP-One HTRF assay in 1321N1 cells stably expressing human PAR2 showed that the IC50 value of AZ3451 was 23nM vs. SLIGRL. The FLIPR assay showed that the IC50 values of AZ3451 were 5.4 nM and 6.6 nM against SLIGRL and trypsin, respectively[1].
作用机制 AZ3451 is an antagonist of PAR2 that binds to a remote allosteric site outside the helical bundle of the receptor, preventing structural rearrangements required for receptor activation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.17mL

8.75mL

1.75mL

0.87mL

17.50mL

3.50mL

1.75mL
参考文献

[1]Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017 May 4;545(7652):112-115.