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Protease-activated Receptor (PAR)

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Cat. No. Product Name Field of Application Chemical Structure
DC41699 FSLLRY-NH2 Featured
FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
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DC73497 TFLLRN-NH2
TFLLRN-NH2 is a potent, PAR1-selective agonist peptide with EC50 of 1.9 uM.
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DC73496 NRD-21
NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.
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DC73495 1-Piperidine Propionic Acid
1-Piperidine Propionic Acid (1-PPA) is an allosteric Inhibitor of protease activated receptor-2 (PAR2) with IC50 of 2.3 uM.
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DC11923 BMS-986120 Featured
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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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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DC7197 ML 161 Featured
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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DC10879 AZ3451 Featured
AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2)
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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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DC71997 BMS-986141
BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.
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DC70677 PAR2 antagonist C391
PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.C391 blocks both PAR2 Ca2+ and MAPK signalling pathways activated by peptidomimetics and/or proteinase activation.C391 effectively attenuated compound 48/80-induced thermal hyperalgesia in vivo.C391 blocked A. alternata-induced, PAR2-dependent Ca2+ and MAPK signalling in 16HBE14o- cells, as well as β-arrestin recruitment in HEK 293 cells.C391 effectively attenuated A. alternata-induced inflammation, mucus production, mucus cell hyperplasia and airway hyperresponsiveness in acute allergen-challenged murine models.
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DC70501 I-287
I-287 is a potent, selective, orally active inhibitor of PAR2, negative PAR2 allosteric modulator, inhibits PAR2-mediated activation of Gq and G12/13 but not Gi/o proteins (IC50=45-390 nM); I-287 is a negative allosteric modulator (NAM) and not an orthosteric competitive antagonist of hPAR2. I-287 inhibits PAR2-mediated activation of DAG/Ca2+/PKC and RhoA/SRF-RE, as well as FAK and ERK1/2 signaling pathways, shows no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization. I-287 inhibits PAR2-induced secretion of IL-8 cytokine in vitro and reduces Freund's adjuvant (CFA)-induced paw edema model in mice.
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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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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.
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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..
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DC46522 Parstatin(mouse) TFA
Parstatin(mouse) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
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DC46521 Parstatin(human) TFA
Parstatin(human) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
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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.
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DC45261 Parstatin(human)
Parstatin(human), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
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DC45260 Parstatin(mouse)
Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
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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.
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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.
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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.
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DC41910 TRAP-6 amide TFA
TRAP-6 amide TFA is a PAR-1 thrombin receptor agonist peptide.
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DC41909 TRAP-6 amide
TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide.
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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.
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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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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.
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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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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.
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