PAR4 antagonist which shows no agonist activity (as measured by platelet aggregation, intracellular Ca2+ release or InsP production). Also inhibits Gαi-coupled formylpeptide FPR2 receptor downstream signaling but does not inhibit downstream signaling of the Gαq-coupled P2Y2 and PAF receptors. Additionally activates the FFAR2 short chain fatty acid receptor. Inhibits platelet aggregation and shows cardioprotective effects by decreasing infarct size before ischemia.Â
References are publications that support the biological activity of the product
The PAR4-derived pepducin P4Pal<sub>10</sub> lacks effect on neutrophil GPCRs that couple to Gαq for signaling but distinctly modulates function of the Gαi-coupled FPR2 and FFAR2.
Holdfeldt A et al (2020) Biochemical pharmacology 180 : 114143