glp-1r modulator-1

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

V-0219 hydrochloride, an orally-active positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R), is utilized in obesity-associated diabetes research.

PF-06372222 is a small-molecule negative allosteric modulator of the glucagon receptor (GCGR). PF-06372222 is also an antagonist for glucagon-like peptide-1 receptor GLP-1R, which inhibits glucagon secretion and glucose-dependent insulin secretion.

GLP-1R modulator L7-028 is a variant that enhances affinity for GLP-1 and (cAMP) signaling.

GLP-1R modulator C5 is a small molecule GLP-1R orthosteric modulator that enhances GLP-1 binding to GLP-1R via transmembrane sites and can be used in the study of type II diabetes.

(R)-V-0219, an enantiomer of V-0219, is an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R). It induces calcium fluxes in HEK cells that stably express hGLP-1R [1].

(S)-V-0219, an enantiomer of V-0219, is an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R). It activates calcium fluxes in HEK cells stably expressing hGLP-1R, demonstrating its oral activity. Additionally, (S)-V-0219 ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice [1].

VU0453379 hydrochloride is a central nervous system (CNS) penetrant and highly selective positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R), demonstrating efficacy with an EC50 of 1.3 μM [1].

(R)-V-0219 hydrochloride, an enantiomer of V-0219, functions as an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R). It induces calcium fluxes in HEK cells expressing hGLP-1R [1], highlighting its biochemical activity and potential therapeutic applications.

(S)-V-0219 hydrochloride, an enantiomer of V-0219, serves as an orally active positive allosteric modulator (PAM) of the GLP-1 Receptor (GLP-1R), enhancing calcium fluxes in HEK cells that stably express hGLP-1R. Additionally, it effectively reduces high glucose levels and suppresses feeding behavior in fasted mice [1].

LSN3160440 is an allosteric modulator of GLP-1R that functions as a protein-protein interaction (PPI) stabilizer or molecular glue, aiding in the binding of inactive GLP-1 (9-36) NH2 to GLP-1R, thereby enhancing receptor activation and potential therapeutic effects [1] [2].