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PZ-128
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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.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Anti-Cancer Compound Library | Anti-Cardiovascular Disease Compound Library | TRAP-6 | AZ3451 | PAR-4 Agonist Peptide, amide TFA | SCH79797 dihydrochloride | Protease-Activated Receptor-2, amide | ENMD-1068 hydrochloride | SLIGRL-NH2 | TFLLR-NH2(TFA) | GB-110 hydrochloride | 2-Furoyl-LIGRLO-amide | AC-55541 | FSLLRY-NH2 TFA | Protease-Activated Receptor-4 | Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA | tcY-NH2 TFA | AC-264613 | Atopaxar | PAR 4 (1-6) (TFA) | Parstatin(human) | Parstatin(mouse) | Protease-Activated Receptor-1, PAR-1 Agonist | RWJ-56110 dihydrochloride | tcY-NH2 | TRAP-6 amide
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热门标签:P1pal-7