| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Mebrofenin targets the hepatobiliary system. As a 99mTc-labeled iminodiacetic acid (IDA) derivative, it is taken up by hepatocytes and excreted into the bile, allowing visualization of the liver, gallbladder, and bile ducts. The compound does not have a classical receptor target but is used for functional imaging of the hepatobiliary system.
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| ln Vitro |
Tc-99m Mebrofenin is a 99mTc-labeled iminodiacetic acid (IDA) derivative that was initially used to detect biliary disorders and, more recently, to measure liver function [3].
In vitro, Mebrofenin is characterized by its ability to chelate technetium-99m for diagnostic imaging. The compound's labeling efficiency and stability with 99mTc are assessed. Its binding to serum proteins and hepatocyte uptake can be studied in vitro using liver cell lines or hepatocyte preparations. The compound's physicochemical properties, including its lipophilicity and protein binding, are characterized. |
| ln Vivo |
In vivo, Mebrofenin is used as a hepatobiliary imaging agent. Following intravenous administration of 99mTc-labeled Mebrofenin, the compound is rapidly taken up by hepatocytes and excreted into the bile. Imaging is performed using a gamma camera to assess liver function, gallbladder emptying, and bile duct patency. It is used clinically for the diagnosis of acute cholecystitis and other biliary disorders.
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| Enzyme Assay |
In vitro assays for Mebrofenin typically involve radiolabeling studies with technetium-99m. The compound is incubated with 99mTc-pertechnetate and a reducing agent (e.g., stannous chloride) under controlled conditions. Labeling efficiency and radiochemical purity are measured by TLC or HPLC. Stability studies assess the compound's integrity in various buffers and biological fluids. Hepatocyte uptake studies can be performed using primary hepatocytes or liver cell lines.
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| Cell Assay |
For in vitro cell-based assays, hepatocytes or liver cell lines are cultured and treated with 99mTc-labeled Mebrofenin. Cellular uptake is measured by counting cell-associated radioactivity. The compound's transport mechanisms can be studied using inhibitors of organic anion transporting polypeptides (OATPs) or other hepatocyte transporters. Cell viability is assessed by standard assays.
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| Animal Protocol |
In vivo animal studies with Mebrofenin are typically conducted in rodents or other animal models to evaluate hepatobiliary function. 99mTc-labeled Mebrofenin is administered intravenously, and dynamic imaging is performed using a gamma camera or SPECT. The compound's biodistribution, hepatic uptake, and biliary excretion are quantified. The effects of various disease states or drug treatments on hepatobiliary function can be assessed.
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| ADME/Pharmacokinetics |
Mebrofenin (CAS: 78266-06-5) has a molecular weight of 387.24 g/mol and a molecular formula of C15H19BrN2O5. It is also known as (3-bromo-2,4,6-trimethylphenylcarbamoyl)methyliminodiacetic acid. Melting point: 192-196°C. Storage: room temperature. It is a diagnostic radiopharmaceutical precursor used for hepatobiliary imaging.
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| Toxicity/Toxicokinetics |
Mebrofenin is a diagnostic agent and is not intended for therapeutic use. As a radiopharmaceutical precursor, its toxicity is related to the radiation exposure from the 99mTc label rather than the chemical compound itself. The unlabeled compound has low pharmacological toxicity. It is used in very small quantities for diagnostic imaging. Contraindications include hypersensitivity to the compound.
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| References |
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| Additional Infomation |
Mebufenone is an amino acid amide.
Mebrofenin is a diagnostic agent used as a 99mTc-labeled hepatobiliary imaging agent for cholescintigraphy. It is used to evaluate liver and biliary tract function, including the diagnosis of acute cholecystitis. It is also known as (3-bromo-2,4,6-trimethylphenylcarbamoyl)methyliminodiacetic acid and has the CAS number 78266-06-5. It is an approved diagnostic radiopharmaceutical in many countries. |
| Molecular Formula |
C15H19N2O5BR
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|---|---|
| Molecular Weight |
387.22576
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| Exact Mass |
386.048
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| CAS # |
78266-06-5
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| PubChem CID |
54158
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| Appearance |
White to off-white solid powder
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| Density |
1.5766 (rough estimate)
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| Boiling Point |
577.4ºC at 760 mmHg
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| Melting Point |
193-198ºC
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| Flash Point |
303ºC
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| Index of Refraction |
1.6520 (estimate)
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| LogP |
1.857
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
443
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(C)=C(NC(CN(CC(O)=O)CC(O)=O)=O)C(C)=C1Br
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| InChi Key |
MHPZZZZLAQGTHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H19BrN2O5/c1-8-4-9(2)15(10(3)14(8)16)17-11(19)5-18(6-12(20)21)7-13(22)23/h4H,5-7H2,1-3H3,(H,17,19)(H,20,21)(H,22,23)
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| Chemical Name |
2-[[2-(3-bromo-2,4,6-trimethylanilino)-2-oxoethyl]-(carboxymethyl)amino]acetic acid
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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 |
| 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 : ~250 mg/mL (~645.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.37 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 20.8 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: ≥ 2.08 mg/mL (5.37 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 20.8 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: ≥ 2.08 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5824 mL | 12.9122 mL | 25.8244 mL | |
| 5 mM | 0.5165 mL | 2.5824 mL | 5.1649 mL | |
| 10 mM | 0.2582 mL | 1.2912 mL | 2.5824 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.