NOTA-GZP
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.
For research use only. We do not sell to patients.
- CAS No.: 2171121-32-5
- Formula: C51H71N11O17S
- Molecular Weight:1142.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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.
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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Molecular Weight 1142.24
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Formula C51H71N11O17S
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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
NOTA-β-Ala-Gly-Gly-Ile-Glu-Phe-Asp-CHO
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Sequence Shortening
NOTA-β-AGGIEFD-CHO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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