Összes fotó(1)
Fontos dokumentumok
SML2050
AZ3451
≥98% (HPLC)
Szinonimák:
2-(6-Bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]-1H-benzimidazole-5-carboxamide
Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez
Összes fotó(1)
About This Item
Tapasztalati képlet (Hill-képlet):
C30H27BrN4O3
CAS-szám:
Molekulatömeg:
571.46
UNSPSC kód:
51111800
NACRES:
NA.77
Javasolt termékek
Teszt
≥98% (HPLC)
form
powder
szín
white to beige
oldhatóság
DMSO: 2 mg/mL, clear
tárolási hőmérséklet
2-8°C
SMILES string
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
Alkalmazás
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.
Biokémiai/fiziológiai hatások
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.
Tárolási osztály kódja
11 - Combustible Solids
WGK
WGK 3
Lobbanási pont (F)
Not applicable
Lobbanási pont (C)
Not applicable
Analitikai tanúsítványok (COA)
Analitikai tanúsítványok (COA) keresése a termék sarzs-/tételszámának megadásával. A sarzs- és tételszámok a termék címkéjén találhatók, a „Lot” vagy „Batch” szavak után.
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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
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