| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Pimonidazole targets hypoxic cells. It is a 2-nitroimidazole derivative that is selectively reduced and binds to macromolecules in hypoxic cells. Under hypoxic conditions, the nitro group is reduced to reactive intermediates that covalently bind to cellular proteins and DNA. This selective binding allows for the detection and quantification of hypoxia in tissues. It also has potential radiosensitizing activities.
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| ln Vitro |
When the oxygen content is less than 1.3%, the 2-nitroimidazole chemical known as pinimadazole, an exogenous hypoxia marker, establishes covalent connections with cellular macromolecules. Detection: Using mouse monoclonal antibodies for immunohistochemistry detection of pimonidazole, hypoxic cells are identified. A proliferating cell nuclear antigen (PCNA) monoclonal antibody that is sold commercially was used to identify cell proliferation. Light microscopy was used to qualitatively evaluate hypoxia and cell proliferation, and point counting and image analysis software techniques were used to quantitatively evaluate the two.
Pimonidazole is not evaluated for direct pharmacological activity in conventional cell-based assays. Its primary use is as a hypoxia marker. In vitro, it is used to detect hypoxic cells in culture. Cells are incubated with Pimonidazole under hypoxic or normoxic conditions, and binding is detected by immunohistochemistry using anti-Pimonidazole antibodies. Its selectivity for hypoxic cells has been extensively characterized. |
| ln Vivo |
Pimonidazole is used in vivo as a hypoxia marker in tumor research. It is administered systemically and selectively binds to hypoxic tissues. It is used to study tumor microenvironments and assess the efficacy of cancer therapies. It is under investigation for the diagnosis of prostate cancer and head and neck cancer. Its ability to detect hypoxia has been validated in preclinical and clinical studies.
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| Enzyme Assay |
Pimonidazole does not have established receptor binding assay protocols. Its activity as a hypoxia marker is assessed by immunohistochemical detection. Physical properties: molecular weight 254.29 g/mol; molecular formula C11H18N4O3; IUPAC name: 1-(2-nitroimidazol-1-yl)-3-piperidin-1-ylpropan-2-ol; purity: typically 98%; appearance: solid. No specific biochemical assay protocols are applicable.
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| Cell Assay |
Cellular hypoxia detection is performed using Pimonidazole in cell culture. Cells are cultured under hypoxic conditions (typically 1% O2) or normoxic conditions and incubated with Pimonidazole at concentrations of 100-500 µM for 1-4 hours. Cells are then fixed and stained with anti-Pimonidazole antibodies. Binding is detected by fluorescence microscopy, flow cytometry, or immunohistochemistry. Hypoxic fractions are quantified by measuring the intensity of Pimonidazole staining. Each experiment includes hypoxic and normoxic controls.
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| Animal Protocol |
In vivo studies are conducted in tumor-bearing mice or other animal models. Pimonidazole is administered intraperitoneally or intravenously at doses typically ranging from 10-60 mg/kg. After 1-4 hours, tumors or other tissues are harvested and fixed. Pimonidazole binding is detected by immunohistochemistry using anti-Pimonidazole antibodies. Hypoxic fractions are quantified by image analysis. The distribution of hypoxia within tumors is assessed. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Pimonidazole has a molecular weight of 254.29 g/mol and a molecular formula of C11H18N4O3. Chemical name: α-[(2-Nitro-1H-imidazol-1-yl)methyl]-1-Piperidineethanol. IUPAC name: 1-(2-nitroimidazol-1-yl)-3-piperidin-1-ylpropan-2-ol. Purity: typically 98%. Storage: typically at -20°C. As a hypoxia marker, it is administered systemically and distributes to tissues.
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| Toxicity/Toxicokinetics |
Pimonidazole is generally well-tolerated at the doses used for hypoxia detection. It is not intended for therapeutic use. Standard toxicology studies have been conducted for its use as a diagnostic agent. No significant toxicity has been reported at the doses used for hypoxia imaging. It is under investigation for diagnostic applications in prostate cancer and head and neck cancer.
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| References |
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| Additional Infomation |
Pimonidazole is a C-nitro compound. It is being investigated for use in the diagnosis of prostate and head and neck cancers. Pimonidazole is a 2-nitroimidazole with hypoxia selectivity and potential radiosensitizing activity. In hypoxic environments such as tumors, Pimonidazole is reduced. In hypoxic cells, the reduced Pimonidazole binds to thiol-containing proteins. The resulting complex accumulates in hypoxic tumors, consuming radioprotective thiols and making tumor cells more sensitive to radiotherapy.
Pimonidazole is also known as 1-(2-nitroimidazol-1-yl)-3-piperidin-1-ylpropan-2-ol. It is a 2-nitroimidazole derivative with hypoxic selectivity. It is widely used as a hypoxia marker in biological research and medical applications. It is under investigation for the diagnosis of prostate cancer and head and neck cancer. No regulatory approvals as a therapeutic agent have been reported. |
| Molecular Formula |
C11H18N4O3
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| Molecular Weight |
254.29
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| Exact Mass |
254.137
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| CAS # |
70132-50-2
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| Related CAS # |
Pimonidazole hydrochloride;70132-51-3;Pimonidazole-d10;2468639-37-2
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| PubChem CID |
50981
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
490.5±55.0 °C at 760 mmHg
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| Flash Point |
250.5±31.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.642
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| LogP |
1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
278
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WVWOOAYQYLJEFD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H18N4O3/c16-10(8-13-5-2-1-3-6-13)9-14-7-4-12-11(14)15(17)18/h4,7,10,16H,1-3,5-6,8-9H2
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| Chemical Name |
1-(2-nitroimidazol-1-yl)-3-piperidin-1-ylpropan-2-ol
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| Synonyms |
PD126675; Ro 038799; PD 126675
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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) |
H2O : ~1 mg/mL (~3.93 mM)
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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 | 3.9325 mL | 19.6626 mL | 39.3252 mL | |
| 5 mM | 0.7865 mL | 3.9325 mL | 7.8650 mL | |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9325 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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