Parmodulin 2_product_DataBase

Bioactivity

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].

Target

IC50: 0.26 μM (PAR1)

Invitro

Parmodulin 2 (ML161; 10 µM; for 30 minutes) inhibits proinflammatory signaling in endothelial HUVECs cells[3].

In Vivo

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]. Animal Model:

Name

Parmodulin 2

CAS

423735-93-7

Formula

C17H17BrN2O2

Molar Mass

361.23

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

Parmodulin 2

CAS: 423735-93-7 F: C17H17BrN2O2 W: 361.23