Orforglipron

Description

Orforglipron Overview

Orforglipron (LY3502970) is a non-peptide, small-molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R) developed by Eli Lilly and Company. Unlike peptide-based GLP-1 receptor ligands, this compound is structurally designed as an orally bioavailable small molecule, allowing investigation of GLP-1 receptor signaling through a non-peptidic scaffold in experimental systems.

In investigational research environments, Orforglipron has been examined in in vitro assays and preclinical research models to evaluate activation of GLP-1 receptor–mediated signaling pathways. The compound is frequently used in experimental models of metabolic pathway regulation, where researchers analyze receptor binding characteristics, intracellular signaling cascades, and ligand–receptor interactions associated with GLP-1R activation.

Chemical and Molecular Properties

Property	Verified Data
Compound Name	Orforglipron
Synonyms	LY3502970; LY-3502970
PubChem CID	137319706
Structure
CAS Number	2212020-52-3
Molecular Formula	C₄₈H₄₈F₂N₁₀O₅
Molecular Weight	883.0 g/mol
IUPAC Name	3-[(1S,2S)-1-[5-[(4S)-2,2-dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one
Solubility	Soluble in methanol (reported in chemical databases)
Storage Conditions	Typically stored at −20 °C in controlled laboratory environments
Reported Purity (research material)	≥95% (analytical grade material commonly used in laboratory research)

Working Mechanism

Receptor Binding and Activation

Orforglipron interacts with GLP-1R and stabilizes an active receptor conformation, enabling coupling with intracellular G proteins.

cAMP Signaling Pathway Activation

Following receptor activation, adenylate cyclase activity may increase, leading to elevated intracellular cyclic adenosine monophosphate (cAMP) levels. This signaling cascade is widely used in laboratory assays to quantify receptor activation.

Downstream Intracellular Signaling

Increased cAMP concentrations can activate protein kinase A (PKA) and other downstream mediators, which regulate transcriptional and metabolic signaling pathways in experimental cell systems.

Regulation of Hormonal Signaling Pathways in Experimental Models

GLP-1 receptor activation influences signaling networks associated with glucagon secretion pathways, pancreatic signaling cascades, and gastrointestinal motility regulation in controlled research models.

Central Nervous System Receptor Signaling (Experimental Models)

Preclinical investigations have explored GLP-1R signaling in neural tissues involved in metabolic regulation. These studies focus on receptor distribution and intracellular signaling dynamics rather than physiological outcomes.

Research Applications in Laboratory Settings

GLP-1 Receptor Pharmacology Studies

Researchers use Orforglipron in in vitro receptor-binding and activation assays to investigate GLP-1R structure-function relationships and ligand-binding characteristics.

Signal Transduction Experiments

The compound is employed in experimental cell models to analyze cAMP-dependent signaling pathways, receptor internalization dynamics, and GPCR downstream signaling networks.

Metabolic Pathway Investigations in Preclinical Models

In preclinical research models, Orforglipron is studied as a tool for examining GLP-1 receptor involvement in metabolic regulatory pathways, including glucagon signaling and pancreatic endocrine signaling mechanisms.

Comparative Ligand Studies

Because it is structurally distinct from peptide-based GLP-1 receptor agonists, Orforglipron allows researchers to perform comparative studies between peptide and non-peptide GLP-1R ligands, helping to clarify receptor activation mechanisms.

Drug Discovery and GPCR Structural Research

Orforglipron has also been used in investigational research to explore structure-activity relationships (SAR) and ligand optimization strategies within GLP-1 receptor drug discovery programs.

Why Choose Purerawz for Orforglipron?

Buy Orforglipronfor laboratory research use from our online shop. At Purerawz, we provide high-quality reference materials. Each research compound comes with a Certificate of Analysis for verification of purity and concentration.

Disclaimer

This information is for educational purposes only and not medical advice. Products are for research use only. Research must follow IRB or IACUC guidelines. Verify information independently before purchasing. By ordering, you agree to our Terms and Conditions. If you are not 100% satisfied with the product you received, please contact us at support@staging.purerawz.co

Reference Links

• Lutkemeyer, C., Pasqualotto, E., Ferreira, R. O. M., Chavez, M. P., Petris, I., Santos, H. V. D., Wille, J. M., Hohl, A., Ronsoni, M. F., & Van De Sande-Lee, S. (2024). Effects of once-daily oral orforglipron on weight and metabolic markers: a systematic review and meta-analysis of randomized controlled trials. Archives of Endocrinology and Metabolism, 68, e230469. https://doi.org/10.20945/2359-4292-2023-0469 
• Dutta, D., Nagendra, L., Anne, B., Kumar, M., Sharma, M., & Kamrul–Hasan, A. B. M. (2024). Orforglipron, a novel non–peptide oral daily glucagon–like peptide–1 receptor agonist as an anti–obesity medicine: A systematic review and meta–analysis. Obesity Science & Practice, 10(2), e743.https://doi.org/10.1002/osp4.743