PZ-128

PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects[1][2][3][4].

Product Specifications

CAS Number

[371131-16-7]

Product Name Alternative

P1pal-7

UNSPSC

12352209

Hazard Statement

H302, H315, H319

Target

Protease Activated Receptor (PAR)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pz-128.html

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CCCCCCCCCCCCCCCC(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CC1=CC=CC=C1)=O)=O)=O)=O)=O)=O)=O

Molecular Formula

C55H99N13O9

Molecular Weight

1086.46

Precautions

H302, H315, H319

References & Citations

[1]Anika Agarwal, et al. Targeting a metalloprotease-PAR1 signaling system with cell-penetrating pepducins inhibits angiogenesis, ascites, and progression of ovarian cancer. Mol Cancer Ther. 2008 Sep;7 (9) :2746-57.|[2]Lidija Covic, et al. Protease-Activated Receptor 1 as Therapeutic Target in Breast, Lung, and Ovarian Cancer: Pepducin Approach. Int J Mol Sci. 2018 Jul 31;19 (8) :2237.|[3]Paul A Gurbel, et al. Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease. Arterioscler Thromb Vasc Biol. 2016 Jan;36 (1) :189-97.|[4]Ping Zhang, et al. Suppression of arterial thrombosis without affecting hemostatic parameters with a cell-penetrating PAR1 pepducin. Circulation. 2012 Jul 3;126 (1) :83-91.