ML161 (Parmodulin 2)

Description: ML-161 is a novel and potent allosteric inhibitor of PAR1 (proteinase-activated receptor 1) on platelets with IC50 of 0.26 uM. ML161 has a different selectivity with the reported ALK inhibitor crizotinib. When tested with human platelets, ML161 treatment inhibited the activation of thrombin-induced platelet in a dose-dependent manner by detecting P-selectin expression. When tested with granule secretion, ML161 exhibited a potent inhibition on P-selectin expression in a dose-dependent manner with EC50 value of 0.3uM and also inhibited SFLLRN-induced thrombus formation. ML-161 prevents surface expression of P-selectin induced by the peptide SFLLRN with an IC50 value of 0.26 uM. ML161 inhibited platelet aggregation induced by a PAR1 peptide agonist or by thrombin but not by several other platelet agonists.

References: ACS Med Chem Lett. 2012 Mar 8; 3(3):232-237.