| S8067 |
Vorapaxar (MK-5348)
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Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
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Cell Rep Med, 2025, 6(10):102371
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Cardiovasc Diabetol, 2025, 24(1):323
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J Immunother Cancer, 2024, 12(11)e009805
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| S9744 |
AZ3451
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AZ3451 is a potent antagonist of protease-activated receptor 2 (PAR2) that binds to a remote allosteric site outside the helical bundle with IC50 of 23 nM.
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Front Immunol, 2024, 15:1477072
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| E0102 |
I-191
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I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signalling pathways and functional responses. This compound also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
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Front Immunol, 2024, 15:1477072
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| E4841 |
Vorapaxar sulfate
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Vorapaxar sulfate (SCH 530348 sulfate) is a selective and orally active antagonist of protease-activated receptor (PAR-1), with a Ki value of 8.1 nM. This compound reduces thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
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| S0342 |
Atopaxar
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Atopaxar (E5555, ER-172594-00) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist.
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| S9916 |
SCH79797 dihydrochloride
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SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist, which can inhibit binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM.
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