NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.
NRD-21 is a negative allosteric modulator of TFLLRN-NH2 at PAR1, rather than a simple competitive inhibition.
NRD-21 (10 uM) caused complete inhibition of platelet aggregation in human platelets in the presence of the PAR1/2 agonist SFLLRN-NH2 (1.5 μM).
NRD-21 (10 uM) inhibited TNF-α (25 ng/mL) induced TF expression in HUVEC.
NRD-21 shows slightly improved potency over Parmodulin 2 (Cat. PC-62640, ML161, IC50=0.57 uM), but with much improved plasma stability, making it more suitable for in vivo studies.
