PZ-128 P1pal-7|cas:371131-16-7|西域试剂

PZ-128 P1pal-7,99.47%

产品编号：Bellancom-107146| CAS NO：371131-16-7| 分子式：C₅₅H₉₉N₁₃O₉| 分子量：1086.46

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货号	价格	库存与货期
Bellancom-107146	￥1500.00	杭州北京（现货）
Bellancom-107146	￥2500.00	杭州北京（现货）
Bellancom-107146	￥5000.00	杭州北京（现货）
Bellancom-107146	￥8000.00	杭州北京（现货）
Bellancom-107146	￥12500.00	杭州北京（现货）

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PZ-128 P1pal-7

产品介绍

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。

生物活性

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^[4].

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 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%.

体内研究

西域 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%.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (92.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9204 mL	4.6021 mL	9.2042 mL
5 mM	0.1841 mL	0.9204 mL	1.8408 mL
10 mM	0.0920 mL	0.4602 mL	0.9204 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。