RGNCY-0010 (GPR103 Antagonist)

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The pyroglutamylated RF amide peptide receptor 103 is located in brain areas important for feeding and body weight control. GPR103 agonists play a key role in homeostasis by promoting increased food intake and body mass. GPR103 antagonists may allow obese patients to lower their body mass though appetite reduction. RGNCY-0010 is a potent GPR103 antagonist (IC50 = 0.046 uM).

Systematic Name: (5-bromo-1-methyl-1H-pyrrolo[2,3-c]pyridin-2-yl)(6-((dimethylamino)methyl)-4-methyl-3,4-dihydroisoquinolin-2(1H)-yl)methanone

SMILES: CC1CN(C(C(N2C)=CC3=C2C=NC(Br)=C3)=O)CC4=C1C=C(CN(C)C)C=C4

Molecular Weight: 441.36

Formula: C22H25BrN4O

PMID: 24937104

Reference: Georgsson, Jennie, et al. "GPR103 antagonists demonstrating anorexigenic activity in vivo: Design and development of pyrrolo [2, 3-c] pyridines that mimic the C-terminal Arg-Phe motif of QRFP26." Journal of Medicinal Chemistry 57.14 (2014): 5935-5948.


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Tags: brain, RGNCY-0010, GPR103, Homeostasis, Apetitie