Description
Orforglipron is a non-peptide small molecule glucagon-like peptide-1 receptor (GLP-1R) agonist developed by Eli Lilly and currently in late-stage clinical research (Phase 3 ACHIEVE and ATTAIN programs). Unlike peptide-based GLP-1 receptor agonists such as semaglutide, tirzepatide, and retatrutide — which require injection due to oral peptide instability — orforglipron is a small molecule (~536 Da) designed for oral bioavailability. The compound represents the first credible oral non-peptide GLP-1RA to reach late-stage clinical research and is a research compound of significant interest in academic studies of small-molecule GLP-1R pharmacology, oral GPCR-agonist chemistry, and comparative GLP-1RA structure-activity relationships. Orforglipron has been characterized in published research literature for its allosteric binding mode at the GLP-1 receptor (distinct from the orthosteric peptide-binding site), cAMP signaling cascade activation, and oral pharmacokinetic profile compared to peptide GLP-1RAs. This compound is offered for laboratory research applications only and remains an investigational research compound without regulatory approval.
Benefits (Research Focus)
• GLP-1 receptor pharmacology research — studied as a non-peptide small molecule GLP-1R agonist for receptor pharmacology research
• Allosteric binding chemistry — investigated for distinct allosteric binding mode at the GLP-1R versus orthosteric peptide GLP-1RAs
• Small-molecule GPCR agonist research — explored as a model compound for small-molecule activation of class B (secretin-like) GPCRs
• Comparative GLP-1RA pharmacology — examined alongside peptide GLP-1RAs (semaglutide, tirzepatide, retatrutide) for comparative receptor research
• Oral pharmacokinetic research — researched for small-molecule oral bioavailability characteristics versus injectable peptide GLP-1RAs
What Researchers Look At
• GLP-1 receptor binding affinity, selectivity, and allosteric versus orthosteric binding mode characterization
• cAMP accumulation, PKA activation, and downstream signaling cascade endpoints in cell research models
• Comparative receptor activation profiles versus peptide GLP-1RAs (semaglutide, tirzepatide)
• Small-molecule oral pharmacokinetic characterization in research models
• Comparative pharmacology across the broader GLP-1R agonist research compound class
Quick Specs
• Form: Gelatin capsule
• Strength: 6 mg orforglipron per capsule
• Appearance: Standard pharmaceutical capsule presentation
• Class: Non-peptide small molecule GLP-1R agonist
• Purity: ≥99%
• Identity: MS-verified (per COA)
• Storage: Protect from light
Identity Basics
• Compound: Orforglipron
• Synonyms: LY3502970; OWL-833 (Chugai Pharmaceutical original code); oral non-peptide GLP-1 receptor agonist
• Class: Non-peptide small molecule GLP-1 receptor agonist; allosteric GLP-1R modulator; oral GPCR-agonist research compound
• Originator: Originally discovered by Chugai Pharmaceutical; currently developed by Eli Lilly
• Mechanism: Allosteric agonist at the GLP-1 receptor (distinct binding site from orthosteric peptide GLP-1RAs)
• Formula: C30H29ClFN5O4
• Molecular Weight: ~536.04 g/mol
• CAS: 2212020-52-3
⚠️ Disclaimer
- This product is intended for laboratory research use only.
- Not for human or veterinary use.
- Not approved for diagnostic, therapeutic, or medical applications.
- Investigational research compound — orforglipron remains in active Phase 3 clinical research; not approved by FDA, Health Canada, or any regulatory authority for any indication.
- Handle using appropriate laboratory safety procedures and personal protective equipment.
COA Verification Notice: Even if the capsule label or product image states a certain concentration, always go by the COA for the true verified value. We reference the COA to determine the verified concentration and purity of each batch, regardless of what the label or product image indicates.
Third-Party Testing
• [COA links for the orforglipron 6mg capsule batch to be added once analytical testing is complete]
