371131-16-7
Chemical Structure
PZ-128
Synonym(s): P1pal-7
- CAS No.: 371131-16-7
- Formula:C55H99N13O9
- Molecular Weight:1086.46
IUPAC Name: N-((2S,5S,8S,11S,14S,17S,20S)-1,24-diamino-17-(4-aminobutyl)-2-benzyl-11-(3-guanidinopropyl)-14-(hydroxymethyl)-5-isobutyl-8-methyl-1,4,7,10,13,16,19-heptaoxo-3,6,9,12,15,18-hexaazatetracosan-20-yl)palmitamide
InChIKey: VZRIKWNVDCTBTF-BKGFHLQYSA-N
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
Biological Activity: 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].
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PZ-128 | 99.83% | 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. | ||||||||||||||||||||
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PZ-128 (Standard) | PZ-128 (Standard) (P1pal-7 (Standard)) is the analytical standard of PZ-128 (HY-107146). This product is intended for research and analytical applications. 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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [3]. 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. [Content Brief]
- [4]. 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. [Content Brief]
