| 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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| S9915 |
FSLLRY-NH2 TFA
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FSLLRY-NH2 TFA (FSY-NH2) is a selective protease-activated receptor 2 (PAR2) inhibitor with an ic50 of 50 µM in PAR2-KNRK cells.
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Am J Transl Res, 2024, 16(12):7416-7426
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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 signaling 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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| E4452 |
Trypsin
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Trypsin(Cocoonase) is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. It activates PAR2 and PAR4 and induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. It also promotes cell proliferation and differentiation and can be used in the research of wound healing and neurogenic inflammation.
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| E7046 |
TRAP-6
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TRAP-6 (PAR-1 agonist peptide) is a synthetic hexapeptide (SFLLRN) that acts as a agonist of PAR-1 (protease-activated receptor-1). It also activates GPR15 on T-cells, regulating immune responses by suppressing acute GvHD while maintaining GvT activity.
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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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| E7294 |
TFLLR-NH2
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TFLLR-NH2 is a selective and potent agonist of proteinase-activated receptor 1 (PAR1) with an EC50 of 1.9 μM. It has potential for researching early tumor metastasis and supports early antiplatelet therapy to suppress colorectal cancer spread and improve survival rates.
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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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| E0341 |
IUN76750
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IUN76750 is a PAR-2 signaling pathway inhibitor.
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