| DC10117 |
AC264613
Featured
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AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation. |
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| DC10879 |
AZ3451
Featured
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AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2) |
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| DC11742 |
AZ-8838 |
AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM. |
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| DC11923 |
BMS-986120
Featured
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BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4. |
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| DC8533 |
E5555 hydrobromide |
E5555 shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC values of 0.064 and 0.031 μM respectively. |
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| DC11741 |
GB-110 |
GB-110 is a potent, non-peptidic agonist of PAR2 that selectively induces PAR2-mediated intracellular Ca(2+) release in HT29 cells with EC50 of 0.28 uM. |
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| DC11740 |
GB-88 |
GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM. |
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| DC7197 |
ML 161
Featured
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Inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). Thought to act allosterically. Also inhibits thrombin-induced platelet activation. |
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| DC8860 |
Vorapaxar
Featured
|
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM. |
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| DC40079 |
PZ-128 |
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects. |
|
| DC40104 |
RWJ-56110 dihydrochloride |
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619. RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
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| DC41699 |
FSLLRY-NH2
Featured
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FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor. |
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| DC41700 |
FSLLRY-NH2 TFA
Featured
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FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor. |
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| DC41701 |
tcY-NH2 |
tcY-NH2 is a selective rat PAR4 antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced rat platelet aggregation. |
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| DC41702 |
tcY-NH2 TFA |
tcY-NH2 TFA is a selective rat PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH2-induced rat platelet aggregation. |
|
| DC41755 |
SLIGRL-NH2 TFA |
SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2). |
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| DC41761 |
PAR 4 (1-6) (TFA) |
PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4) and acts as PAR4-specific agonist. |
|
| DC41909 |
TRAP-6 amide |
TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide. |
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| DC41910 |
TRAP-6 amide TFA |
TRAP-6 amide TFA is a PAR-1 thrombin receptor agonist peptide. |
|
| DC42020 |
Protease-Activated Receptor-1, PAR-1 Agonist |
Protease-Activated Receptor-1, PAR-1 Agonist is a thrombin-specific, protease-activated receptor 1 (PAR-1)-specific agonist peptide. |
|
| DC42021 |
Protease-Activated Receptor-3 (PAR-3) (1-6), human |
Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide. |
|
| DC45259 |
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA |
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide. |
|
| DC45260 |
Parstatin(mouse) |
Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis. |
|
| DC45261 |
Parstatin(human) |
Parstatin(human), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis. |
|
| DC45574 |
Protease-Activated Receptor-1, PAR-1 Agonist TFA |
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor. |
|
| DC46521 |
Parstatin(human) TFA |
Parstatin(human) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis. |
|
| DC46522 |
Parstatin(mouse) TFA |
Parstatin(mouse) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis. |
|
| DC47251 |
FR-171113 |
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM.. |
|
| DC47359 |
SCH79797 |
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes. |
|
| DC70391 |
ENMD-1068 hydrochloride |
ENMD-1068 is a novel selective PAR2 antagonist without inhibitory activity against thrombin-mediated PAR3 and PAR4 signaling; blocks TNFα production in synovial explants from patients with arthritis, and inhibits mast cell tryptase-induced recruitment of eosinophils into the pleural cavity of mice, dose dependently attenuates joint inflammation. |
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