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. PAR-1 Antagonist

    Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
  3. PAR2 agonist

    AC-264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5).
  4. PAR1 inhibitor

    ML-161 is an 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).
  5. Thrombin Receptor Activator for Peptide 5 (TRAP-5), coagulation factor II (thrombin) receptor is a G protein-coupled receptor involved in the regulation of thrombotic response.
  6. PAR2 antagonist

    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  7. 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.
  8. PAR2 antagonist

    GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M.
  9. 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).
  10. PAR2 antagonist

    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  11. PAR2 agonist

    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.
  12. TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide.
  13. PAR-1 agonist

    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.
  14. PAR-2 (1-6) (human) (SLIGKV), a peptide ligand, is a PAR-2 agonist.
  15. PAR-1 agonist

    iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 that refers to the use of isoserine instead of serine as first amino acid.
  16. FLLRN is a biological active peptide. (PAR1-specific antagonist peptide)
  17. PAR2 agonist

    AY254 is an analogue of AY77. AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling.
  18. PAR2 agonist

    AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.

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