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PZ-128

CAS No. : 371131-16-7

MCE 站：PZ-128

产品活性：PZ-128 (P1pal-7) 是一种细胞穿透肽，是一种首创的，特异性的且可逆的蛋白酶激活受体 1 (PAR1) 拮抗剂。PZ-128 靶向 PAR1 的细胞质表面，并中断向内部定位 G (PAR1-G) 蛋白的信号。PZ-128 具有抗血小板，抗转移，抗血管生成和抗癌作用。

研究领域：GPCR/G Protein

作用靶点：Protease-Activated Receptor (PAR)

In Vitro: PZ-128 (P1pal-7; 3 μM) blocks 90-94% of OVCAR-4 migration toward human ovarian ascites and fibroblast conditioned media. The OVCAR4-treated peritoneal fibroblast conditioned media elicits a 2.2-fold increase in endothelial barrier permeability which could be nearly completely inhibited by PZ-128.
PZ-128 is a lipidated ‘pepducin’ which targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G proteins. The structure of PZ-128 is found to mimic the off-state of the corresponding intracellular region of PAR1 which is critical for coupling to G proteins.

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.

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