Protease-Activated Receptors (PAR)

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  1. PAR4 antagonist

    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively.
  2. non-peptide PAR2 agonist

    GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  3. PAR2 antagonist

    GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M.
  4. PAR4 antagonist

    UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM).

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