NOTA-GZP
Based on 1 Customer Validation
NOTA-GZP is a high-affinity, specific granzyme B-targeted irreversible inhibitory peptide PET imaging probe. NOTA-GZP can be used for the research of colon carcinoma, melanoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.86%
- CAS No.: 2171121-32-5
- Formule: C51H71N11O17S
- Masse moléculaire:1142.24
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
Non-radioactive gallium-labeled NOTA-GZP (30 min) inhibits activated human granzyme B with a Ki of 47 nM in a cell-free enzyme inhibition assay[1].
68Ga-NOTA-GZP (30 min) exhibits 5-11 fold specificity for activated human granzyme B over other granzyme family members and pro-granzyme B in a cell-free binding assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
68Ga-NOTA-GZP (37 MBq; i.v.; single dose) PET imaging with a mean Tmax of 1.90 in high-uptake tumors completely predicts future tumor regression in combination immunotherapy-treated colon cancer-bearing mice prior to tumor size divergence[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/C mice (immunocompetent)[1]
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Dosage:37 MBq
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Administration:i.v.; single dose
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Result:Showed uptake in tumors, kidneys, and bladder.
Correlated highly with Western blot-quantified granzyme B expression.
Had an average tumor to blood ratio (TBR) of 1.29 in anti-PD-1 treated tumors.
Had an average TBR of 1.83 in combination therapy treated tumors.
Showed significantly elevated TBR above untreated mice (TBR=0.96) in both anti-PD-1 and combination therapy treated groups.
Confirmed PET analysis results via ex vivo gamma counting.\nSplit treated mice into two non-overlapping groups: high GZP uptake and low GZP uptake.
Showed high-uptake group was significantly different from low-uptake group and untreated controls.
Showed no significant TBR difference between low-uptake treated tumors and untreated controls.
Demonstrated equivalent tumor volumes across all groups at imaging time, but all high-uptake tumors subsequently regressed, while all low-uptake tumors progressed.
Chemical Information
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CAS No. 2171121-32-5
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Appearance Solid
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Masse moléculaire 1142.24
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Formule C51H71N11O17S
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Color White to off-white
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SMILES
O=C(NCC(NCC(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC(O)=O)C=O)=O)=O)=O)=O)=O)CCNC(NC(C=C2)=CC=C2CC3CN(CC(O)=O)CCN(CC(O)=O)CCN3CC(O)=O)=S
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Sequence
{p-SCN-Bn-NOTA}-{βAla}-Gly-Gly-Ile-Glu-Phe-Asp-CHO
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Sequence Shortening
{p-SCN-Bn-NOTA}-{βAla}-GGIEFD-CHO
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (43.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.8755 mL | 4.3774 mL | 8.7547 mL | 21.8868 mL |
| 5 mM | 0.1751 mL | 0.8755 mL | 1.7509 mL | 4.3774 mL | |
| 10 mM | 0.0875 mL | 0.4377 mL | 0.8755 mL | 2.1887 mL | |
| 15 mM | 0.0584 mL | 0.2918 mL | 0.5836 mL | 1.4591 mL | |
| 20 mM | 0.0438 mL | 0.2189 mL | 0.4377 mL | 1.0943 mL | |
| 25 mM | 0.0350 mL | 0.1751 mL | 0.3502 mL | 0.8755 mL | |
| 30 mM | 0.0292 mL | 0.1459 mL | 0.2918 mL | 0.7296 mL | |
| 40 mM | 0.0219 mL | 0.1094 mL | 0.2189 mL | 0.5472 mL |
NOTA-GZP Related Classifications
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