2077238-49-2
2077238-49-2
Chemical Structure
GRPR antagonist-3
- CAS No.: 2077238-49-2
- Formula:C33H37FN6O5
- Molecular Weight:616.68
InChIKey: DESMGZJNKKZTEC-YTTGMZPUSA-N
SMILES: O=C(NC1=CC=C(C=C1)[N+]([O-])=O)N[C@](CC2=CNC3=CC=CC=C23)(C)C(NCC4(C5=CC=C(C=N5)OCCF)CCCCC4)=O
Biological Activity: GRPR antagonist-3 (compound (S)-1m) is a potent GRPR antagonist with an IC50 of 121 nM. GRPR antagonist-3 is stable in rat plasma and towards microsomal oxidative metabolism in vitro. GRPR antagonist-3 can be radiolabeled with fluorine-18 for PET imaging[1].
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GRPR antagonist-3 | GRPR antagonist-3 (compound (S)-1m) is a potent GRPR antagonist with an IC50 of 121 nM. GRPR antagonist-3 is stable in rat plasma and towards microsomal oxidative metabolism in vitro. GRPR antagonist-3 can be radiolabeled with fluorine-18 for PET imaging. | |||||||||||||||||||||
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References
- [1]. Lacivita E, et al. Structure-activity relationship study towards non-peptidic positron emission tomography (PET) radiotracer for gastrin releasing peptide receptors: Development of [18F] (S)-3-(1H-indol-3-yl)-N-[1-[5-(2-fluoroethoxy)pyridin-2-yl]cyclohexylmethyl]-2-methyl-2-[3-(4-nitrophenyl)ureido]propionamide. Bioorg Med Chem. 2017 Jan 1;25(1):277-292. [Content Brief]
