|Targets||Protease-Activated Receptors (PARs)|
|Description||UDM-002555 is a small-molecule and selective antagonist of protease-activated receptor-4 (PAR-4). It can suppress the activation of platelet in dose manner. In combination with aspirin, it inhibited arterial thrombosis with limited impact on hemostasis in cynomolgus monkeys.|
|Brife Description||antagonist of PAR-4, resistant to platelet, arterial thrombosis|
|Application||the potential treatment of arterial thrombosis|
|Current Developer||Bristol-Myers Squibb|
AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist which displays no activity at other PAR subtypes or at over 30 other receptors in...
LIGRL-NH2 is a PAR2 activator with EC50 value of ~5 µM. It can be used to explore signaling through PAR2 in cells.
E 5555 hydrobromide
E 5555 hydrobromide is a potent and orally bioactive thrombin receptor (or protease-activated receptor 1, PAR1) antagonist (IC50 = 19 nM). It inhibits human pla...
UDM-002555 is a small-molecule and selective antagonist of protease-activated receptor-4 (PAR-4). It can suppress the activation of platelet in dose manner. In ...
SCH-530348 is a novel antiplatelet agent undergoing development by Schering-Plough Corp for the treatment and prevention of atherothrombosis. It is currently un...
SCH 79797 dihydrochloride
SCH 79797 dihydrochloride is a potent and selective non-peptide PAR1 receptor antagonist (IC50 = 70 nM). SCH 79797 blocks haTRAP-induced human platelet aggregat...
BMS-986141 is a dual antagonist of proteinase-activated receptor 1 (PAR1) and PAR4. BMS-986141 was confirmed in cynomolgus monkeys to be a better therapy for pr...
VKGILS-NH2 is a reversed control peptide for SLIGKV-NH2, which is a protease-activated receptor 2 (PAR2) agonist.
LRGILS-NH is a control peptide for SLIGRL-NH2, a protease-activated receptor-2 (PAR2) agonist that facilitates gastrointestinal transit in vivo.
BMS-986120, an imidazoles derivative, has been found to be a PAR4 antagonist that could probably be effective against thrombus propagation and pathological vasc...
SLIGKV-NH2 is a protease-activated receptor 2 (PAR2) agonist (Ki = 9.64 μM; IC50 = 10.4 μM).
tcY-NH2 is a selective PAR4 antagonist peptide that inhibits aggregation caused by receptor-activating peptide analogs (GY-NH2, AY-NH2) and thrombin.
FR 171113 is a protease-activated receptor 1 (PAR1) antagonist displaying significant antiplatelet activity in vitro. It inhibits thrombin TRAP-6-induced platel...
GB 83 is a selective antagonist of human protease activated receptor 2 (PAR2) (IC50 = 2 mM).
2-Furoyl-LIGRLO-amide is a potent and selective PAR2 receptor agonist (pD2 = 7.0). It causes a dose-dependent relaxation of murine femoral arteries.
ML 354 is a selective PAR4 antagonist with IC50 value of 140 nM.
FSLLRY-NH2 is a selective PAR2 peptide antagonist. It reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice, also suppre...
AC 264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). AC 264613 inhibits interferon regulatory factor 5 and decreases ...
Atopaxar is a Protease-activated receptor-1 (PAR-1) inhibitor. It can inhibit the binding of a high-affinity thrombin receptor-activating peptide ([(3)H]haTRAP)...
Thrombin Receptor Activator Peptide 6
TRAP-6, a peptide compound, has been found to be a PAR1 agonist and could also influence the phosphorylation of rapid phosphodiesterase 3A in the positive way.