L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl- Struktur

L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl-

Bezeichnung:L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl-

Englisch Name:L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl-

CBNumberCB98103124

SummenformelC55H99N13O9

Molgewicht1086.46

L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl- physikalisch-chemischer Eigenschaften

Aggregatzustand	Solid
Farbe	White to off-white

Gefahreninformationscode (GHS)

L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl- Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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].

in vivo

PZ-128 (P1pal-7; 10 mg/kg; intraperitoneal injection; every other day; for 6 weeks) treatment significantly reduces mean ascites fluid volume by 60%. PZ-128 treatment also causes a highly significant 84-96% reduction in blood vessel density in both the center and edge of the OVCAR-4 tumors^[1].

Animal Model:	Female NCR Nu/Nu mice (5-7 weeks) injected with OVCAR-4 or SKOV-3 cells^[1]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; every other day; for 6 weeks
Result:	Significantly reduced mean ascites fluid volume by 60%.

IC 50
PAR1
Einzelnachweise
[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. DOI:10.1158/1535-7163.MCT-08-0177
[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. DOI:10.3390/ijms19082237
[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. DOI:10.1161/CIRCULATIONAHA.112.091918
[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. DOI:10.1161/ATVBAHA.115.306777

L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl- Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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