488097-06-9

VU 0650991 is a non-competitive GLP-1 antagonist that is orally bioavailable and acts as a brain penetrant.

GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM[1].

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[1] Kellie D. Nance, et al. Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione core. J. Med. Chem. 19 Jan 2017. DOI:10.1021/acs.jmedchem.6b01706