LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

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).

GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. It reduces glucose and body weight, and has the potential to be used in Type 2 diabetes mellitus (T2DM) research.

Avexitide (Exendin (9-39)) is a specific and competitive antagonist of glucagon-like peptide-1 (GLP-1) receptor.

Teduglutide (ALX-0600, Gattex, Revestive, TAK 633) is an analogue of human glucagon-like peptide-2 (GLP-2) and binds to the GLP-2 receptors. Teduglutide prolongs the intestinotrophic properties of GLP-2 in animal models.

LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).

V-0219 is a small molecule positive allosteric modulator (PAM) of GLP-1R with Emax of 60% in the cAMP assay.V-0219 potentiated insulin secretion in INS-1 β-cells with EC50 of 0.25 nM, the best response was observed at 0.1 nM, when a fixed concentration of 0.2 nM of GLP-1 was added to the dose-response curve of 9, the maximal response observed reached a plateau at 0.1 nM, with an EC50 value of 0.008 nM.V-0219 shows a remarkable in vivo activity, reducing food intake and improving glucose handling in normal and diabetic rodents.

TT-OAD2 is a potent, selective, non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor with EC50 of 5 nM.TT-OAD2 inhibited GLP-1- and oxyntomodulin-mediated cAMP, calcium, pERK1/2 and β-arrestin responses in a concentration-dependent manner.TT-OAD2 exhibits biased agonism, and kinetics of G-protein activation and signalling that are distinct from peptide agonists.

TT-OAD2 hydrochloride is a potent, selective, non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor with EC50 of 5 nM.TT-OAD2 inhibited GLP-1- and oxyntomodulin-mediated cAMP, calcium, pERK1/2 and β-arrestin responses in a concentration-dependent manner.TT-OAD2 exhibits biased agonism, and kinetics of G-protein activation and signalling that are distinct from peptide agonists.

Cotadutide (MEDI-0382) is a dual GLP-1/glucagon receptor peptide agonist with robust anti-obesity and metabolic effects.

GLP-1R agonist 6 is a potent GLP-1R agonist with an EC50 of 0.15 nM for human GLP-1R (WO2021249492A1, compound 005A or 005B).

GLP-1R agonist 5 is a potent GLP-1R agonist with an EC50 of <10 nM (WO2021259309A1, compound 35).

GLP-1R agonist 7 is a potent GLP-1R agonist with an EC50 of 0.67 µM (WO2021244645A1, compound WXA001).

GLP-1R agonist 8 is a potent GLP-1R agonist with an EC50 of < 2 nM (WO2021219019A1, compound 129a).

GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17).

GLP-1 receptor agonist 9 is a GLP-1 receptor agonist, example 7, extracted from WO2020234726 A1.

GLP-1 receptor agonist 7 is a potent agonist of glucagon-like peptide-1 (GLP-1). GLP-1 receptor agonist 7 has the potential for the research of GLP-1-associated diseases, disorders, and conditions including diabetes mellitus (extracted from patent WO2021219019A1, compound 130b).

LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.

Ecnoglutide is a glucagon-like peptide 1 (GLP-1) receptor agonist.

Utreglutide is a potent glucagon-like peptide 1 (GLP-1) receptor agonit.

glucagon receptor antagonists-4 is a highly potent glucagon receptor antagonist.

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

GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects.

GLP-1(28-36)amide TFA, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide TFA is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide TFA has anti-diabetic and cardioprotection effects.

GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice.

GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice.

GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).