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[1].

Product Specifications

CAS Number

[2077238-49-2]

UNSPSC

12352005

Target

Bombesin Receptor

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer

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

Molecular Formula

C33H37FN6O5

Molecular Weight

616.68

References & Citations

[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.