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アッセイ
≥98% (HPLC)
フォーム
powder
色
white to beige
溶解性
DMSO: 2 mg/mL, clear
保管温度
2-8°C
SMILES記法
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
アプリケーション
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.
生物化学的／生理学的作用
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.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
毒物及び劇物取締法
劇物
Jan Code
SML2050-VAR:
SML2050-BULK:
SML2050-5MG:4548173350288
SML2050-25MG:4548173350271
最新バージョンのいずれかを選択してください：
試験成績書（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
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
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
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
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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