Orforglipron: Scientific Profile
Publicado el · Actualizado el
Non-peptide GLP-1 receptor agonist, small molecule and orally administered.
Orforglipron (English name Orforglipron; development code LY3502970; CAS 2212020-52-3) is a synthetic, orally administered compound belonging to the class of glucagon-like peptide-1 receptor (GLP-1R) agonists. Its distinctive feature is that it is NOT a peptide but a small non-peptide molecule, which allows it to be orally active without the absorption and stability limitations inherent to peptide incretin analogs. It was developed by Eli Lilly.
Orforglipron's mechanism of action is based on agonism of the GLP-1 receptor, a class B G protein-coupled receptor. By activating this pathway, in research models it reproduces the effects of incretin signaling also mediated by peptide analogs: potentiation of glucose-dependent insulin secretion, slowing of gastric emptying, and modulation of satiety circuits. Its experimental interest lies in the fact that, being a small orally administered non-peptide molecule, it offers an alternative route to injectable peptides for the study of GLP-1 signaling.
In the research setting, Orforglipron is used as a tool for studying the GLP-1 receptor, glucose homeostasis, and energy metabolism through oral non-peptide agonism, and as a comparator against peptide incretin analogs in cell and animal models.
Orforglipron is supplied in the presentation indicated for its stable storage, protected from light and moisture according to the protocol. This product is offered exclusively as a research reagent (research use only): it is not intended for the diagnosis, prevention or treatment of any disease, nor for human or veterinary consumption.
Clinical Studies (5)
- Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity (Wharton, et al. · The New England Journal of Medicine · 2023) PMID 37351564.
- Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist, in Early Type 2 Diabetes (Rosenstock J, et al. · The New England Journal of Medicine · 2025) PMID 40544435.
- Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment (Wharton S, et al. · The New England Journal of Medicine · 2025) PMID 40960239.
- Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study (Frias, et al. · The Lancet · 2023) PMID 37369232.
- Orforglipron (LY3502970), a novel, oral non-peptide glucagon-like peptide-1 receptor agonist: A Phase 1a, blinded, placebo-controlled, randomized, single- and multiple-ascending-dose study in healthy participants (Pratt, et al. · Diabetes, Obesity & Metabolism · 2023) PMID 37344954.
Technical data
- CAS
- 2212020-52-3
- Molecular formula
- C48H48F2N10O5
- Molecular weight
- 883 Da
- Compound type
- small_molecule
- Light-sensitive
- No
Frequently asked questions about Orforglipron
What is Orforglipron?
Non-peptide GLP-1 receptor agonist, small molecule and orally administered.
What are the chemical properties of Orforglipron?
Molecular formula C48H48F2N10O5; molecular weight 883 Da; CAS number 2212020-52-3.
What routes of administration are studied for Orforglipron?
In the research models the following are described: subcutaneous. Use is exclusively for scientific research.
