AZ3451 - Protease-Activated Receptor (PAR) Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAZ3451Cat. No.: HY-112558CAS No.: 2100284-59-9分式: CHBrNO分量: 571.46作靶点: Protease-Activated Receptor (PAR)作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 83.3 mg/mL (145.77

2、 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.64 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.64 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 AZ3451蛋酶激活受体-2 (protease-activated receptor-2 (PAR2) 拮

3、抗剂，IC50 值为 23 nM。IC50 & Target Protease-activated receptor-2 (IC50= 23 nM) 1体外研究 Antagonist AZ3451 binds to a remote allosteric site outside the helical bundle of the protease-activatedreceptor 2. AZ3451 is highly lipophilic, which coincides with the hydrophobic nature of the binding pocketwithin th

4、e membrane. Antagonist binding prevents structural rearrangements required for receptor activationand signalling 1.REFERENCES1. Cheng RKY, et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017 May 4;545(7652):112-115.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;Fax: 02