| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
p‑NH2‑Bn‑NOTA targets biomolecules (antibodies, peptides) via its para‑amino benzyl group, which can be activated to a maleimide or NHS ester for conjugation. The NOTA cage chelates trivalent radiometals such as ⁶⁸Ga, ⁶⁶Ga, and ⁸⁹Zr with exceptionally high kinetic inertness and thermodynamic stability. The complexation kinetics of NOTA with gallium are faster than DOTA at room temperature.
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| ln Vitro |
In vitro, p‑NH2‑Bn‑NOTA is used to conjugate to targeting vectors. A typical protocol: p‑NH2‑Bn‑NOTA (1 mg) is dissolved in 100 microL anhydrous DMSO, then added to a 5 mg/mL peptide solution in 0.1 M HEPES buffer (pH 8.5) in the presence of NHS and EDC. After 2 h at RT, the conjugate is purified by HPLC, and the chelator‑to‑peptide ratio is determined by MS. Radiolabeling with ⁶⁸Ga achieves >97% radiochemical purity in 10 min at RT.
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| ln Vivo |
p‑NH2‑Bn‑NOTA is not directly used in animals. The ⁶⁸Ga‑labeled NOTA‑peptide conjugate (5-15 MBq) is injected intravenously into tumor‑bearing mice. PET/CT imaging shows high target‑specific uptake (SUV 5-15) and rapid renal clearance. NOTA conjugates exhibit lower non‑specific liver uptake compared to DOTA conjugates due to less lipophilicity. The ⁸⁹Zr‑labeled NOTA‑antibody conjugates show excellent in vivo stability.
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| Enzyme Assay |
Metal chelation is tested in a cell‑free system. p‑NH2‑Bn‑NOTA (10 microM) is incubated with ⁶⁸GaCl3 (eluted from ⁶⁸Ge/⁶⁸Ga generator, 0.05 M HCl, 5 microL) in 200 microL 0.5 M HEPES buffer (pH 4.0‑5.5) at RT for 10 min. Radiochemical yield is measured by radio‑ITLC using silica gel strips and 0.1 M citrate buffer (pH 5) as mobile phase. Labeling efficiency ≥98% is typical. Stability is tested in human serum at 37 degC for 2 h.
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| Cell Assay |
No direct assay is performed. For a peptide‑NOTA conjugate, cells (5×10⁵, receptor‑positive) are incubated with ⁶⁸Ga‑labeled NOTA‑peptide (1 nM, 0.5 nCi) in binding buffer at 4 degC for 1 h. Non‑specific binding is determined with a 100‑fold excess of unlabeled peptide. Cells are washed three times with ice‑cold PBS, and bound radioactivity is counted. Specific binding typically exceeds 85% of total bound counts.
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| Animal Protocol |
For animal evaluation, ⁶⁸Ga‑NOTA‑peptide (100 microL, 10-15 MBq) is injected via tail vein into mice bearing receptor‑positive subcutaneous tumors (e.g., U87MG for RGD or PC‑3 for bombesin). Dynamic PET scans are performed for the first 60 min, followed by static scans at 1 h and 2 h post‑injection. Tumor uptake is calculated as %ID/g. NOTA conjugates show high contrast images with low background signal.
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| ADME/Pharmacokinetics |
The NOTA chelator forms a very stable ⁶⁸Ga complex with fast kinetics. After injection of ⁶⁸Ga‑NOTA‑peptide, plasma half‑life is 1-2 h, with predominantly renal excretion of the intact peptide. The parent chelator has no inherent PK properties. The complex is stable in blood and urine, with <5% transchelation at 2 h post‑injection. The labelled peptide is metabolized in the lysosomes of target cells.
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| Toxicity/Toxicokinetics |
p‑NH2‑Bn‑NOTA is a laboratory reagent, not a drug. Toxicity data are not available for the chelator alone. However, NOTA and its metal complexes are considered biocompatible with low intrinsic toxicity. The free chelator may be a skin and eye irritant. Handle with standard precautions (gloves, goggles, fume hood). The compound is not for human use.
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| Additional Infomation |
p‑NH2‑Bn‑NOTA is not an approved drug. It is a research‑only bifunctional chelator for PET imaging agent development, particularly for ⁶⁸Ga‑ and ⁸⁹Zr‑labeled probes. Its fast radiolabeling kinetics and high in vivo stability make it a chelator of choice for ⁶⁸Ga‑based PET tracers. It is used for labeling peptides, small molecules, and antibodies for imaging cancer, inflammation, and other diseases.
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| Molecular Formula |
C19H34CL2N4O8
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|---|---|
| Molecular Weight |
517.40
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| Appearance |
White to off-white solid powder
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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 | 1.9327 mL | 9.6637 mL | 19.3274 mL | |
| 5 mM | 0.3865 mL | 1.9327 mL | 3.8655 mL | |
| 10 mM | 0.1933 mL | 0.9664 mL | 1.9327 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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