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NRD-21

Chemical Structure : NRD-21

CAS No.: 2403529-11-1

NRD-21

Catalog No.: PC-20576Not For Human Use, Lab Use Only.

NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 386.21
Formula C17H12BrN3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(C1=CN=CO1)NC2=CC=CC(NC(C3=CC=CC=C3Br)=O)=C2

References

1. Disha M Gandhi, et al. Bioorg Med Chem. 2019 Sep 1;27(17):3788-3796.

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