par4, human

BMS-986120 is a first-in-class oral, reversible protease-activated receptor 4 (PAR4) antagonist with IC50s of 9.5 nM in human blood and 2.1 nM in monkey blood, exhibiting potent and selective antiplatelet effects[1][2].

Compound 12, a PAR4 antagonist6, exhibits inhibitory activity with IC50 values of 134 nM and 150 nM against hPAR4 and mPAR4, respectively.

PAR4 antagonist8 (Compound 20f) is an effective oral and selective PAR4 antagonist with an IC50 of 15.32 nM, boasting favorable pharmacokinetic properties. It effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50=6.39 nM) and also suppresses platelet aggregation in mice. PAR4 antagonist8 is utilized in anti-thrombotic research.

PAR4 antagonist3 (Compound 36) is a selective antagonist of protease-activated receptor 4 (PAR4). It exhibits antiplatelet activity with an IC50 of 26.1 nM and enhances metabolic stability in human liver microsomes, with a half-life (T1/2) of 97.6 minutes.

PAR4 antagonist4 (Compound 37) is a selective antagonist of protease-activated receptor 4 (PAR4). It exhibits antiplatelet activity with an IC50 of 14.2 nM. Moreover, PAR4 antagonist3 enhances metabolic stability in human liver microsomes, showing a half-life (T1/2) of 42.5 minutes.

PAR4 antagonist 2 (Compound 31) is a protease-activated receptor 4 (PAR4) antagonist with IC50 values of 95 nM for human PAR4 and 367 nM for mouse PAR4. It inhibits the activation of PAR4 through cleavage by the natural protease thrombin but has no effect on the synthetic PAR4 agonist peptide AYPGKF.

PAR-4 (1-6) amide human, an N-terminal fragment of protease-activated receptor 4 (PAR4), induces platelet aggregation [1].