For research use only. Not for therapeutic Use.
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM[1]. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo[2].
Parmodulin 2 (ML161; 10 µM; for 30 minutes) inhibits proinflammatory signaling in endothelial HUVECs cells[3].
Parmodulin 2 (ML161; 5 mg/kg; IV) significantly inhibits platelet thrombus formation, with a 73% inhibition in AUC (area under the curve)[2].
Parmodulin 2 inhibits platelet thrombus formation in vivo, and it does not prolong bleeding time. Parmodulin 2 selectively inhibits platelet aggregation through Par1 and the α2A-adrenergic receptor[2].
| Catalog Number | R059270 |
| CAS Number | 423735-93-7 |
| Synonyms | 2-bromo-N-[3-(butanoylamino)phenyl]benzamide |
| Molecular Formula | C17H17BrN2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H17BrN2O2/c1-2-6-16(21)19-12-7-5-8-13(11-12)20-17(22)14-9-3-4-10-15(14)18/h3-5,7-11H,2,6H2,1H3,(H,19,21)(H,20,22) |
| InChIKey | DFOVLSMXPWPCFH-UHFFFAOYSA-N |
| SMILES | CCCC(=O)NC1=CC(=CC=C1)NC(=O)C2=CC=CC=C2Br |
| Reference | [1]. Gandhi DM, et al. Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells. Bioorg Med Chem. 2018 May 15;26(9):2514-2529. [2]. Susanna F Gunnink, et al. Allosteric inhibition of protease activated receptor 1: a new antiplatelet therapy. [3]. Aisiku O, et al. Parmodulins inhibit thrombus formation without inducing endothelial injury caused by vorapaxar. Blood. 2015 Mar 19;125(12):1976-85. |
