Glucagon-Like Peptide 1 Receptor Agonist II

A pyrimidine small molecule that acts as a GLP-1 allosteric agonist that induces cAMP signaling in HEK293 cells expressing the GLP-1 receptor with EC₅₀ = 0.66 µM and 99% efficacy (similar data with rat GLP-1 receptor), does not compete with radiolabelled GLP-1 in receptor binding assays, and is not active in cells expressing the GLP-2, GIP, PTH, or glucagon receptors. In rodent islets, insulin secretion increases in a dose-dependent and glucose-dependent manner, either alone or in an additive fashion when combined with the endogenous GLP-1 peptide. In vivo, this molecule exhibits insulinotropic effects when dosed at 10mg/kg in SD rats undergoing an IVGTT and a hyperglycemic clamp. It is also shown to increase insulin secretion in perifusion assays involving normal and diabetic human islets ex vivo, at concentrations between 1 and 10 µM.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sloop, KW., et al. 2010. Diabetes.59, 3099.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany