计算溶液所需的质量、体积或浓度。
PZ-128, 蛋白酶激活受体 1 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NCR Nu/Nu mice (5-7 weeks) injected with OVCAR-4 or SKOV-3 cells Dosage: 10 mg/kg Administration: Intraperitoneal injection; every other day; for 6 weeks Result: Significantly reduced mean ascites fluid volume by 60%.
IC50& Target:PAR1
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
PZ-128
生化机理
PZ-128（P1pal-7）是一种细胞穿透性脂肽蛋白肽，是第一类特异性可逆蛋白酶激活受体-1（PAR1）拮抗剂。PZ-128 以 PAR1 的细胞质表面为靶点，中断向内部定位的 G（PAR1-7）发出信号。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
蛋白酶激活受体 1 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N
关联CAS
PubChem CID
MeSH Entry Terms
P1pal-7;PZ-128 peptide
分子量
1086.46
技术文档
高级数据
产品属性
| ALogP | 4.9 |
|---|
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 371131-16-7，分子式为 C55H99N13O9，分子量为 1086.46 g/mol。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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