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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Exametazime targets the brain's regional cerebral blood flow by forming a lipophilic complex with ⁹⁹ᵐTc that can cross the blood-brain barrier. Once in the brain, the complex is converted to a hydrophilic form that is trapped in the brain tissue, allowing for imaging of regional cerebral perfusion. As a chelating agent, it forms a cationic complex with the radioactive isotope technetium-99m. It can also be used for the labeling of leukocytes to localize intra-abdominal infections and inflammatory bowel disease.
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| ln Vitro |
In vitro, Exametazime is recognized as an effective leukocyte labeling agent. The compound forms a stable complex with ⁹⁹ᵐTc that is lipophilic and can cross cell membranes. The ⁹⁹ᵐTc-Exametazime complex is used for in vitro leukocyte labeling in medical diagnostics. The racemate form is the chemical standard for this radiopharmaceutical preparation. Specific in vitro activity data are not typically reported as the compound is a diagnostic agent rather than a therapeutic drug.
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| ln Vivo |
In vivo, ⁹⁹ᵐTc-Exametazime is used for regional cerebral perfusion imaging in nuclear medicine. After intravenous injection, the lipophilic complex crosses the blood-brain barrier and is distributed in the brain according to regional blood flow. The compound is used to detect altered regional cerebral perfusion in stroke and other cerebrovascular diseases. It is also used for the labeling of leukocytes to localize intra-abdominal infections and inflammatory bowel disease. The radiopharmaceutical is sold under the trade name Ceretec.
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| Enzyme Assay |
The radiopharmaceutical preparation of ⁹⁹ᵐTc-Exametazime involves mixing Exametazime with a solution containing ⁹⁹ᵐTc-pertechnetate. The chelation reaction forms a neutral, lipophilic ⁹⁹ᵐTc-Exametazime complex. The radiochemical purity is assessed by thin-layer chromatography or HPLC. For leukocyte labeling, isolated leukocytes are incubated with the ⁹⁹ᵐTc-Exametazime complex, and labeling efficiency is measured. Quality control includes testing for radiochemical purity and sterility.
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| Cell Assay |
Cellular assays for Exametazime involve leukocyte labeling studies. Leukocytes are isolated from whole blood and incubated with ⁹⁹ᵐTc-Exametazime at 37°C for 15-30 minutes. Labeling efficiency is determined by measuring the radioactivity associated with the cell pellet compared to the total radioactivity. Cell viability is assessed using trypan blue exclusion. The labeled leukocytes are used for in vivo migration studies to detect sites of infection or inflammation.
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| Animal Protocol |
In vivo imaging studies with ⁹⁹ᵐTc-Exametazime are performed in patients or animal models. The radiopharmaceutical is administered intravenously, and images are acquired using a gamma camera or SPECT (single-photon emission computed tomography). For cerebral perfusion imaging, images are acquired 10-30 minutes after injection. For infection imaging, images are acquired at various time points after injection of labeled leukocytes. Image analysis includes visual assessment and quantitative regional uptake measurements.
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| ADME/Pharmacokinetics |
As a diagnostic radiopharmaceutical, the pharmacokinetics of ⁹⁹ᵐTc-Exametazime are well characterized. After intravenous injection, the lipophilic complex rapidly crosses the blood-brain barrier and is distributed according to regional cerebral blood flow. The complex is converted to a hydrophilic form in the brain and is trapped, allowing for imaging. The compound is rapidly cleared from the blood with a half-life of minutes. The ⁹⁹ᵐTc label has a physical half-life of 6 hours. Renal excretion is the primary route of elimination.
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| Toxicity/Toxicokinetics |
The radiation dose from ⁹⁹ᵐTc-Exametazime is within acceptable limits for diagnostic nuclear medicine procedures. As a radiopharmaceutical, the compound is administered in tracer amounts, and the radiation exposure is carefully controlled. Non-radioactive Exametazime is generally well-tolerated at the doses used for radiopharmaceutical preparation. Allergic reactions are rare. The compound is contraindicated in pregnancy and breastfeeding. Standard radiation safety precautions apply when handling and administering the radiopharmaceutical.
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| References |
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 |
Eccrine is a ketoxime compound. It is a diagnostic radiopharmaceutical, commonly used in the preparation of Tc99m eccrine 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 racemate (HM-PAO) is a lipophilic agent that forms a ⁹⁹ᵐTc complex for brain perfusion imaging. It is used for detecting altered regional cerebral perfusion in stroke and cerebrovascular diseases and for leukocyte labeling to detect infections. Marketed as Ceretec. For diagnostic use only. |
| 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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| Related CAS # |
Exametazime
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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,
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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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