| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Gadopentetate dimeglumine does not have a traditional pharmacological target. Its mechanism of action is physical. As a paramagnetic agent, it contains a gadolinium ion with seven unpaired electrons, which creates a strong magnetic moment. When injected intravenously, it distributes in the vascular and extracellular spaces. The paramagnetic gadolinium ion shortens the T1 and T2 relaxation times of nearby water protons, leading to an increase in signal intensity on T1-weighted MRI images.
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| ln Vitro |
Gadofibrate dimeglumine was compared to gadopentetate dimeglumine-enhanced MRI, mammography, and ultrasonography in a cohort of patients selected due to inconclusive results from conventional imaging or who received breast MRI for preoperative staging. The rate of cancer detection has increased dramatically with enhanced MRI [1]. In healthy mice, lymphatic routes were clearly shown by interstitial MR lymphography using gadopentetate dimeglumine (Gd-DTPA) or gadolate disodium (Gd-EOB-DTPA), with no discernible changes between the two medications. The distinction. However, because of their quick kinetics, the imaging time window is limited, which encourages several assessments within a single imaging session [2]. Gaudopentetate dimeglumine spills from the gastrointestinal tract can be directly observed to distinguish ischemia in this paradigm from control rats [3].
In vitro, Gadopentetate dimeglumine is used as a reference standard and in quality control for MRI contrast agents. Its relaxivity, a measure of its ability to shorten T1 relaxation time, is measured in aqueous solutions. The compound is not typically used in cell-based pharmacological assays, as its mechanism of action is physical and does not involve receptor or enzyme interactions. |
| ln Vivo |
In vivo, Gadopentetate dimeglumine is a widely used contrast agent for MRI. It is administered intravenously and distributes in the vascular and extracellular spaces. It is used to enhance the visibility of lesions with abnormal vascularity in the brain, spine, and head and neck. It is commonly employed in neurological, cardiovascular, and oncological imaging. Its use allows for better visualization of tumors, inflammation, and other pathologies.
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| Enzyme Assay |
For in vitro assays, the primary parameter measured for Gadopentetate dimeglumine is its relaxivity. This is determined by measuring the T1 relaxation time of water protons in solutions containing varying concentrations of the compound using a relaxometer or an MRI scanner. The relaxivity (r1) is calculated from the slope of the relaxation rate (1/T1) versus concentration plot. This assay is used to characterize the contrast-enhancing properties of the compound.
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| Cell Assay |
Gadopentetate dimeglumine is not typically used in standard cell-based pharmacological assays. Its effect is physical and does not involve cellular receptors or signaling pathways. However, its cellular uptake and distribution can be studied in vitro using cell culture models, where its concentration in cells can be measured by ICP-MS (inductively coupled plasma mass spectrometry).
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| Animal Protocol |
In vivo, the efficacy of Gadopentetate dimeglumine as a contrast agent is evaluated in animal models or in clinical trials. The compound is administered intravenously, and MRI scans are performed at various time points. The signal enhancement in target tissues is measured, and the pharmacokinetic parameters, such as distribution and clearance, are determined.
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| ADME/Pharmacokinetics |
Gadopentetate dimeglumine (CAS 86050-77-3) has a molecular formula of C14H20GdN3O10·2(C7H17NO5) and a molecular weight of 938.00 g/mol. It is a white to off-white crystalline powder, odorless, slightly sweet, and very soluble in water. It contains 16.76% gadolinium. Storage: typical for contrast agents (protected from light, room temperature). Purity: typically ≥97% for research use.
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| Toxicity/Toxicokinetics |
Gadopentetate dimeglumine has a well-established clinical safety profile. It is generally safe, but serious adverse reactions, including nephrogenic systemic fibrosis (NSF), have been associated with the use of gadolinium-based contrast agents in patients with severe renal impairment. Its toxicity is primarily related to the potential release of free gadolinium ions, which are toxic. The chelation with DTPA reduces this risk.
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| References |
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| Additional Infomation |
Гадопентетат димеглумин является одобренным FDA рецептурным препаратом для использования в качестве контрастного вещества при МРТ. Он продается под торговой маркой Magnevist. Это один из первых контрастных веществ на основе гадолиния. Его механизм действия заключается в сокращении времени релаксации T1, что улучшает контрастность изображений МРТ. Он используется в широком спектре диагностических визуализационных исследований.
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| Molecular Formula |
C28H54GDN5O20
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| Molecular Weight |
938.0
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| Exact Mass |
938.26
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| CAS # |
86050-77-3
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| Appearance |
White to off-white solid powder
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| SMILES |
[C@@H](O)([C@@H](O)CNC)[C@H](O)[C@H](O)CO.O=C1C[N+]23CC[N+]45CC(O[Gd+3]6724(OC(=O)C5)(OC(=O)C[N+]6(CC3)CC(O7)=O)O1)=O.[H+]
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~106.61 mM)
H2O : ≥ 100 mg/mL (~106.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (53.30 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0661 mL | 5.3305 mL | 10.6610 mL | |
| 5 mM | 0.2132 mL | 1.0661 mL | 2.1322 mL | |
| 10 mM | 0.1066 mL | 0.5330 mL | 1.0661 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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