NOTA-MAL-Cys39-Exendin-4
NOTA-MAL-Cys39-Exendin-4 is an imaging agent and radiotracer precursor targeting GLP-1R. NOTA-MAL-Cys39-Exendin-4 binds specifically to GLP-1R and is rapidly cleared by the liver and spleen during the blood pool phase. NOTA-MAL-Cys39-Exendin-4 can be efficiently radiolabeled with gallium-68 to form a stable radiotracer with high radiochemical purity. NOTA-MAL-Cys39-Exendin-4 is applicable to research related to insulinomas.
For research use only. We do not sell to patients.
- Formula: C202H309N55O66S2
- Molecular Weight:4628.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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GLP-1 |
[68Ga]Ga-NOTA-MAL-Cys39-Exendin-4 (37 kBq/well; 15-120 min at 37°C) is taken up by INS-1 rat insulinoma cells, reaching a stable plateau of 4.81 %AD by 60 min, with uptake significantly reduced by excess unlabeled Cys39-exendin-4 (1 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old, insulinoma xenograft model)[1]
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Dosage:3.7 MBq; 0.74 MBq
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Administration:i.v. via tail vein
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Result:Reached a tumor uptake plateau of 12 %ID/g within 5 minutes, remained at 12 %ID/g at 30 minutes, 12 %ID/g at 60 minutes, and 11 %ID/g at 120 minutes post-injection.
Confirmed tumor uptake of 12 %ID/g at 15 minutes, 12 %ID/g at 30 minutes, 12 %ID/g at 60 minutes, and 11 %ID/g at 120 minutes post-injection via biodistribution studies.
Achieved tumor-to-blood, tumor-to-muscle, and tumor-to-pancreas ratios of 30.64, 40.21, and 6.46, respectively, at 60 minutes post-injection.
Reduced tumor uptake to 0.52 %ID/g (imaging) and 1 %ID/g (biodistribution) at 60 minutes post-injection when excess unlabeled Cys39-exendin-4 was administered prior.
Chemical Information
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Molecular Weight 4628.07
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Formula C202H309N55O66S2
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SMILES
O=C(NCC(N[C@@H](CCC(O)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H]([C@H](O)C)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCSC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](C)C(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC3=CNC4=CC=CC=C34)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CC(N)=O)C(NCC(NCC(N5[C@@H](CCC5)C(N[C@@H](CO)C(N[C@@H](CO)C(NCC(N[C@@H](C)C(N6[C@@H](CCC6)C(N7[C@@H](CCC7)C(N(CCC8)[C@@H]8C(N[C@H](C(N)=O)CSC9C(N(CCNC(CN(CCN%10CC(O)=O)CCN(CC%10)CC(O)=O)=O)C(C9)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC%11=CNC=N%11)N
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Sequence
His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Cys(Mal-NOTA)-NH2
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Sequence Shortening
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPP-Cys(Mal-NOTA)-NH2
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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)