FGLP21
FGLP21 is a polypeptide targeting FGL1. FGLP21 has a simulated binding affinity of -9.56 kcal/mol for FGL1, and inhibits the binding of 68Ga-NODA-FGLP21 to FGL1 in a competitive binding assay using FGL1-positive Huh7 cells, with an IC50 of 101.0 nM. FGLP21 preferentially binds to FGL1-positive Huh7 cells, and excess unlabeled FGLP21 can significantly block the uptake of 68Ga-NODA-FGLP21 in Huh7 xenograft tumors. FGLP21 can be used for FGL1-targeted tumor imaging and immune checkpoint research.
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- Fòrmula: C48H84N18O13
- Peso molecular:1121.29
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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FGL1 101 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Huh-7 | IC50 |
101.0 nM
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Inhibition of 68Ga-NODA-FGLP21 binding to human Huh7 hepatocarcinoma cells assessed via competitive cell-binding assay with co-incubation of unlabeled FGLP21 for 2 h at 37 °C, measured by γ counter of cell-associated radioactivity.
Inhibition of 68Ga-NODA-FGLP21 binding to human Huh7 hepatocarcinoma cells assessed via competitive cell-binding assay with co-incubation of unlabeled FGLP21 for 2 h at 37 °C, measured by γ counter of cell-associated radioactivity.
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39893698 |
FGLP21 exhibits a simulated binding affinity of -9.56 kcal/mol for purified FGL1 protein via hydrogen bonding between specific peptide and protein residues[1].
Biotin-labeled FGLP21 (8 μg/mL; 2 h) binds specifically to FGL1-positive Huh7 human hepatocarcinoma cells, as evidenced by strong fluorescence signals, but shows minimal binding to FGL1-negative U87 MG human glioma cells[1].
Unlabeled FGLP21 (0.01 nM-100 μM; 2 h) inhibits the binding of 68Ga-NODA-FGLP21 to FGL1-positive Huh7 human hepatocarcinoma cells with an IC50 of 101.0 nM, indicating specific binding to FGL1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh7 human hepatocarcinoma cells (FGL1-positive), U87 MG human glioma cells (FGL1-negative)
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Concentration:8 μg/mL (biotin-labeled FGLP21); 1:300 dilution (PE-conjugated streptavidin)
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Incubation Time:2 h; SA-PE: additional 1 h
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Result:Produced strong fluorescence signals in Huh7 cells.
Detected low fluorescence signals in U87 MG cells.
68Ga-NODA-FGLP21 (5.0 MBq; intravenous injection; single dose) shows extremely low accumulation in FGL1-negative U87 MG xenografts, with a tumor uptake of only 0.82% ID/g in biodistribution studies at 30 minutes post-injection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG mice (6-8 weeks old)[1]
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Dosage:5.0 MBq (tracer); 10 mg/kg (unlabeled, blocking studies)
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Administration:i.v.; single dose
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Result:Reached tumor uptake of 3.21% ID/g with a tumor-to-muscle ratio of 19.40 at 30 minutes post-injection in microPET imaging.
Achieved tumor uptake of 2.51% ID/g with a tumor-to-muscle ratio of 19.40 at 60 minutes post-injection in microPET imaging.
Reduced tumor uptake to 1.17% ID/g at 30 minutes post-injection and 0.81% ID/g at 60 minutes post-injection when co-injected with unlabeled FGLP21 in microPET imaging.
Reached tumor uptake of 3.48% ID/g with a tumor-to-blood ratio of 2.37 and tumor-to-muscle ratio of 17.85 at 30 minutes post-injection in biodistribution studies.
Achieved tumor uptake of 2.85% ID/g with a tumor-to-blood ratio of 8.08 and tumor-to-muscle ratio of 21.5 at 60 minutes post-injection in biodistribution studies.
Reached tumor uptake of 1.70% ID/g with a tumor-to-blood ratio of 16.5 and tumor-to-muscle ratio of 32.5 at 120 minutes post-injection in biodistribution studies.
Reduced biodistribution tumor uptake to 0.94% ID/g at 30 minutes post-injection when co-injected with unlabeled FGLP21.
Detected no significant radioactivity (<2% ID/g) in normal organs except kidneys.
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Animal Model:NCG mice (6-8 weeks old)[1]
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Dosage:5.0 MBq
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Administration:i.v.; single dose
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Result:Reached tumor uptake of 0.83% ID/g at 30 minutes post-injection in microPET imaging.
Achieved tumor uptake of 0.46% ID/g at 60 minutes post-injection in microPET imaging.
Reached tumor uptake of 0.82% ID/g with a tumor-to-blood ratio of 0.70 and tumor-to-muscle ratio of 4.20 at 30 minutes post-injection in biodistribution studies.
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Animal Model:BALB/c mice (6-8 weeks old)[1]
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Dosage:18.5 MBq
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Administration:i.v.; single dose
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Result:Observed no macroscopic lesions or significant histopathological damage in major organs (heart, liver, spleen, lung, kidney) compared to the saline control group.
Chemical Information
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Peso molecular 1121.29
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Fòrmula C48H84N18O13
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Sequence
Ala-Ala-Val-His-Leu-Arg-Asp-Arg-Ala-Leu
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Sequence Shortening
AAVHLRDRAL
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGLP21 Related Classifications
HY-P11932 Related Classifications
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