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Gd-PCTA-Ach 是一种具有高动力学惰性和中等白蛋白亲和力的大环类钆基 MRI 造影剂。Gd-PCTA-Ach 与白蛋白的结合特性有效延长了血液循环时间。Gd-PCTA-Ach 主要通过肾脏清除,同时约 10% 的剂量经由肝胆途径排泄,呈现出独特的双通道排泄特征。Gd-PCTA-Ach 能够实现对脑部和肝脏肿瘤病灶的高质量成像,在肝癌及胶质瘤的诊断研究中具有重要的应用价值。

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Gd-PCTA-Ach

Gd-PCTA-Ach Chemical Structure

CAS No. : 3031550-73-6

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  • 生物活性

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生物活性

Gd-PCTA-Ach is a macrocyclic gadolinium-based MRI contrast agent with high kinetic inertness and moderate albumin affinity. The albumin-binding property of Gd-PCTA-Ach effectively prolongs its blood circulation time. Gd-PCTA-Ach is mainly cleared via the kidneys, while approximately 10% of the dose is excreted through the hepatobiliary pathway, exhibiting a unique dual-channel excretion profile. Gd-PCTA-Ach enables high-quality imaging of brain and liver tumor lesions, and has important application value in diagnostic studies of liver cancer and glioma[1].

体外研究
(In Vitro)

Gd-PCTA-Ach (0.5-400 mM; 24 h, 37 °C, 5% CO2) 表现出可忽略的细胞毒性,在 HEK-293、AML-12 和 C8-D1A 细胞中,经 0.5 至 400 mM 浓度处理 24 h 后,细胞存活率仍保持在 80% 以上[1]

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

Cell Viability Assay[1]

Cell Line: HEK-293 (human embryonic kidney), AML-12 (mouse hepatocyte), C8-D1A (mouse astrocyte) cells
Concentration: 0.5-400 mM
Incubation Time: 24 h (37 °C, 5% CO2)
Result: Maintained cell viability above 80% for all cell lines across all tested concentrations.
体内研究
(In Vivo)

Gd-PCTA-Ach (0.1 mmol [Gd]/kg;静脉注射;单次推注给药) 可在小鼠多个器官中产生持久、强烈的对比增强效果,经成像和生物分布分析证实,其主要通过肾脏排泄 (约 90%),部分经肝胆排泄 (约 10%)[1]
Gd-PCTA-Ach (0.1 mmol [Gd]/kg;静脉注射;单次推注给药) 可在小鼠体内实现原位肝细胞癌的清晰显像,注射后 3 min 和 30 min 时肝-肿瘤 CNR 均出现具有统计学意义的升高[1]
Gd-PCTA-Ach (0.1 mmol [Gd]/kg;静脉注射;单次推注) 在小鼠体内的肝脏摄取部分由 OATP 转运体介导,因为预先给予 OATP 抑制剂溴磺酞 (HY-D0217) 可显著降低肝脏增强水平并提高肾脏增强水平[1]
Gd-PCTA-Ach (0.05-0.1 mmol [Gd]/kg;静脉注射;单次推注) 可在小鼠中实现有效的脑肿瘤显影,在 0.1 mmol [Gd]/kg 剂量下性能更优,且在 0.05 mmol [Gd]/kg 的低剂量下显影增强效果与对照试剂相当[1]

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

Animal Model: BALB/c mice (male, 9 weeks old, 25-30 g)[1]
Dosage: 0.1 mmol [Gd]/kg
Administration: i.v.; single bolus injection
Result: Produced strong, prolonged contrast enhancement in the heart, liver, kidney, and aorta for 1 h post-injection.
At 5 min post-injection, reached a liver parenchyma ΔSNR 2.4-fold higher than that of a comparator agent, remaining stable at ~60% of a hepatobiliary control agent's level from 20 to 60 min post-injection.
Showed 21% Gd accumulation in the kidney at 30 min, 4.7% in the liver at 30 min, and 0.65% in the bile duct at 30 min, with 1.2% Gd remaining in blood at 15 min.
Achieved full clearance by 24 h post-injection.
Animal Model: BALB/c nude mice (male, 6 weeks old, orthotopic hepatocellular carcinoma xenograft model)[1]
Dosage: 0.1 mmol [Gd]/kg
Administration: i.v.; single bolus injection
Result: Made the tumor margin clear at 3 min post-injection, with a liver-to-tumor CNR 1.35-fold higher than pre-injection values.
Showed slight intratumoral enhancement at 3 min post-injection, which decreased by 30 min post-injection due to vascular washout; the liver-to-tumor CNR remained 1.36-fold higher than pre-injection values at 30 min.
分子量

1042.28

Formula

C44H66GdN7O12

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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产品名称:
Gd-PCTA-Ach
目录号:
HY-182045
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