推荐产品
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
N#CC1=CC=C(NC(C2=CC=C(N([C@H](C3CCCCC3)C)C(C4=CC(OCO5)=C5C=C4Br)=N6)C6=C2)=O)C=C1
InChI key
FJAOGFGHTPYADT-SFHVURJKSA-N
应用
AZ3451 has been used as a protease-activated receptor 2 (PAR-2) antagonist to study the involvement of PAR-2 receptors in factor X activated (FXa)-induced upregulation of the cell adhesion molecules.
生化/生理作用
AZ3451 exhibits anti-inflammatory function in vivo. It can be used as a potential therapeutic for osteoarthritis (OA).
AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2), a G protein-coupled receptor thought to be involved in inflammatory diseases, pain, allergic associated diseases (eosinophil migration, mast cells) and cancers. AZ3451 was found to bind to a remote allosteric site outside the helical bundle that is different from the site previously found on PAR1, and had an IC50 value of 23 nM. AZ3451 was able to completely inhibit ERK phosphorylation when added to 1321N1 cells overexpressing wild-type human PAR2.
Allosteric antagonist of protease-activated receptor 2 (PAR2)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
R Schneckmann et al.
Basic research in cardiology, 118(1), 31-31 (2023-08-15)
Pharmacological inhibition of factor Xa by rivaroxaban has been shown to mediate cardioprotection and is frequently used in patients with, e.g., atrial fibrillation. Rivaroxaban's anti-inflammatory actions are well known, but the underlying mechanisms are still incompletely understood. To date, no
Robert K Y Cheng et al.
Nature, 545(7652), 112-115 (2017-04-27)
Protease-activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) that are irreversibly activated by proteolytic cleavage of the N terminus, which unmasks a tethered peptide ligand that binds and activates the transmembrane receptor domain, eliciting a cellular cascade in
Xiaojian Huang et al.
Aging, 11(24), 12532-12545 (2019-12-17)
Osteoarthritis (OA) is a highly prevalent joint disorder blamed for pain and disability in older individuals. It's commonly accepted that inflammation, apoptosis, autophagy and cellular senescence participate in the progress of OA. Protease activated receptor 2 (PAR2), a member of
Cristina Almengló et al.
Biochemical pharmacology, 178, 114063-114063 (2020-06-04)
We aimed to study the effects of the new oral anticoagulant edoxaban, a factor X activated (FXa) inhibitor, on key endothelial functions that could contribute to cardiovascular benefit. Human umbilical endothelial cells (HUVEC) were obtained from donated umbilical cords and
Amanda J Kennedy et al.
Communications biology, 3(1), 782-782 (2020-12-19)
Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule tractability and a complex activation mechanism. Here we report the pharmacological profiling of a potent new agonist, suggested by molecular modelling
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