| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| Targets |
Exametazime does not have a specific pharmacological target; it is a lipophilic chelator that forms a complex with technetium-99m for diagnostic imaging. The 99mTc-exametazime complex crosses the blood-brain barrier and is trapped in brain tissue in proportion to regional cerebral blood flow. This allows for the assessment of cerebral perfusion using SPECT imaging. The compound's lipophilicity is essential for its ability to cross cellular membranes and the blood-brain barrier.
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| ln Vitro |
In vitro, exametazime has been studied for its ability to form stable complexes with 99mTc and for its lipophilicity. The radiochemical purity and stability of the 99mTc-exametazime complex are characterized by chromatography methods. The compound's ability to cross cellular membranes is assessed in cell-based uptake studies. These in vitro studies ensure the quality and reproducibility of the radiopharmaceutical preparation.
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| ln Vivo |
In vivo, the 99mTc-exametazime complex is used for cerebral perfusion imaging in humans. Following intravenous injection, the complex crosses the blood-brain barrier and is distributed in brain tissue in proportion to regional cerebral blood flow. SPECT imaging is performed to visualize and quantify cerebral perfusion. Exametazime is used in the diagnosis and assessment of various neurological conditions, including stroke, dementia, epilepsy, and cerebral ischemia.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable for exametazime as it is a diagnostic imaging agent rather than a drug that targets specific enzymes or receptors. However, radiochemical purity and stability assays are performed to ensure the quality of the 99mTc-exametazime complex. These assays include thin-layer chromatography, high-performance liquid chromatography, and other analytical methods to measure the radiochemical purity and stability of the complex.
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| Cell Assay |
In vitro cellular studies with exametazime are limited, as it is a diagnostic agent rather than a therapeutic compound. However, cell-based uptake studies may be performed to characterize the ability of the 99mTc-exametazime complex to cross cellular membranes. These studies use cultured cells and measure the uptake of radiolabeled complex by gamma counting or autoradiography.
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| Animal Protocol |
In vivo animal experiments with exametazime are performed in the context of radiopharmaceutical development and validation. Animals are administered the 99mTc-exametazime complex intravenously, and biodistribution studies are performed to determine the tissue distribution of the radiolabeled complex. SPECT imaging in animal models is used to validate the imaging properties of the compound. These studies ensure the safety and efficacy of exametazime for clinical use.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of exametazime include its lipophilicity, which enables it to cross cellular membranes and the blood-brain barrier. The compound has a molecular weight of 272.39 g/mol and molecular formula C13H28N4O2. The 99mTc-exametazime complex is rapidly cleared from the blood and distributed to the brain, with peak brain uptake occurring within minutes after injection. The compound is primarily eliminated via the kidneys.
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| Toxicity/Toxicokinetics |
Toxicological data for exametazime are derived from its use as a diagnostic radiopharmaceutical. The compound is administered in small amounts for imaging purposes and has a favorable safety profile. Adverse reactions are rare and generally mild. The compound is contraindicated in patients with hypersensitivity to exametazime or any of its components. As with all radiopharmaceuticals, the benefits of the examination should outweigh the potential risks of radiation exposure.
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| References |
[1]. Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD):
National Library of Medicine (US); 2006–. Technetium Tc 99m Exametazime.
2020 Oct 19. PMID: 30000634.
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| Additional Infomation |
Exametazime is a ketoxime compound. It is a diagnostic radiopharmaceutical, commonly used in the preparation of Tc99m Exametazime injection. As a chelating agent, it forms a cationic complex with the radioactive isotope technetium-99m. It is used to detect changes in localized cerebral perfusion and for radiolabeling of autologous leukocytes.
Exametazime is also known as HMPAO, Hexametazime, Hexametazine, and Hexamethylpropylene amine oxide. It is a lipophilic compound that forms a neutral, lipophilic complex with 99mTc for cerebral perfusion imaging. The 99mTc-exametazime complex is used in SPECT to assess regional cerebral blood flow in various neurological conditions including stroke, dementia, epilepsy, and cerebral ischemia. It is a diagnostic radiopharmaceutical and is not intended for therapeutic use. |
| Molecular Formula |
C13H28N4O2
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|---|---|
| Molecular Weight |
272.38702
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| Exact Mass |
272.221
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| CAS # |
105613-48-7
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| PubChem CID |
9552071
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| Appearance |
Typically exists as solid at room temperature
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| Melting Point |
128-130°
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| LogP |
2.45
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
19
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| Complexity |
297
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O/N=C(/[C@H](NCC(CN[C@@H](/C(=N/O)/C)C)(C)C)C)\C
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| InChi Key |
BPNZYADGDZPRTK-UDUYQYQQSA-N
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| InChi Code |
InChI=1S/C13H28N4O2/c1-9(11(3)16-18)14-7-13(5,6)8-15-10(2)12(4)17-19/h9-10,14-15,18-19H,7-8H2,1-6H3/b16-11+,17-12+/t9-,10-/m1/s1
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| Chemical Name |
2-Butanone, 3,3'-((2,2-dimethyl-1,3-propanediyl)diimino)bis-, dioxime, (R*,R*-(E,E))-(+-)-
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| Synonyms |
dlHM-PAO dl-HM-PAO dl HM-PAOhexamethylpropyleneamineoxime HMPAO
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6712 mL | 18.3560 mL | 36.7121 mL | |
| 5 mM | 0.7342 mL | 3.6712 mL | 7.3424 mL | |
| 10 mM | 0.3671 mL | 1.8356 mL | 3.6712 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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