GCGR Modulator

NNC-0640 is an effective negative allosteric modulator (NAM) of the human glucagon receptor (GCGR), with an IC₅₀ value of 69.2 nM. NNC-0640 holds potential for research in the field of diabetes.

LSN3318839 is an orally active positive modulator of the glucagon-like peptide-1 receptor (GLP-1R). LSN3318839 can increase the secretion of insulin and has the effect of lowering blood sugar.

VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC₅₀ value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes.

GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC₅₀ 1.59 ± 0.53 μM).

GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC₅₀ 11.01 ± 2.73 μM).

GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC₅₀ 8.43 ± 3.82 μM).

GPCR modulator-1 is a negative allosteric modulator of the GLP-1 receptor (GLP-1R). GPCR modulator-1 can be used for the study of type 2 diabetes.

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

TP-α (TPG-456) is a glucagon-selective two-photon fluorescent probe with a K_d of 65 μM. TP-α directly interacts with glucagon to produce significant fluorescence enhancement. TP-α selectively stains viable glucagon-secreting α cells in pancreatic islets, enabling visualization of their localization, distribution and availability. TP-α is applicable to diabetes research (Ex/Em = 370nm/510 nm).