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  3. Gd-PCTA-Ach

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.

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Gd-PCTA-Ach

Gd-PCTA-Ach Chemical Structure

CAS No. : 3031550-73-6

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Description

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].

In Vitro

Gd-PCTA-Ach (0.5-400 mM; 24 h, 37 °C, 5% CO2) exhibits negligible cytotoxicity, with cell viability remaining above 80% in HEK-293, AML-12, and C8-D1A cells after 24 h incubation at concentrations ranging from 0.5 to 400 mM[1].

MedChemExpress (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.
In Vivo

Gd-PCTA-Ach (0.1 mmol [Gd]/kg; i.v.; single bolus injection) provides prolonged, strong contrast enhancement in multiple mouse organs, with primary renal excretion (~90%) and partial hepatobiliary excretion (~10%) confirmed via imaging and biodistribution analysis[1].
Gd-PCTA-Ach (0.1 mmol [Gd]/kg; i.v.; single bolus injection) enables clear visualization of orthotopic hepatocellular carcinoma in mice, with a statistically significant increase in liver-to-tumor CNR at both 3 min and 30 min post-injection[1].
Gd-PCTA-Ach (0.1 mmol [Gd]/kg; i.v.; single bolus injection) hepatic uptake in mice is partially mediated by OATP transporters, as preadministration of the OATP inhibitor bromosulfophthalein (HY-D0217) significantly reduces liver enhancement and increases renal enhancement[1].
Gd-PCTA-Ach (0.05-0.1 mmol [Gd]/kg; i.v.; single bolus injection) provides effective brain tumor contrast in mice, with superior performance at 0.1 mmol [Gd]/kg and equivalent enhancement to a comparator agent at a reduced dose of 0.05 mmol [Gd]/kg[1].

MedChemExpress (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.
Molecular Weight

1042.28

Formula

C44H66GdN7O12

CAS No.
SMILES

O=C([O-]1)C(CCC(NC2CCCCC2O)=O)[N@@]34CC[N@@]5(C(C([O-]6)=O)CCC(NC7CCCCC7O)=O)CC8=CC=CC9=[N]8[Gd+3]351%106[N@@](CC4)(C(C([O-]%10)=O)CCC(NC%11CCCCC%11O)=O)C9

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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