Orforglipron Research Compound (Non-Peptide GLP-1 Receptor Agonist) Supplier — UPOR Biotech
Orforglipron (LY3502970) — first-in-class, non-peptide, orally bioavailable small-molecule GLP-1 receptor agonist (CAS 2673951-35-7). Unlike peptide GLP-1RAs that require injection, orforglipron is a synthetic small molecule absorbed intact from the GI tract for once-daily oral dosing without food or water restrictions. A partial agonist with biased signaling and a distinct binding mode at GLP-1R. Research-grade (RUO) compound for type 2 diabetes, obesity, and oral GLP-1 drug discovery from UPOR Biotech.
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Orforglipron (CAS 2673951-35-7, C₄₈H₄₈F₂N₁₀O₅, MW 882.97 g/mol) — also known as LY3502970 — is a first-in-class, non-peptide, orally bioavailable small-molecule GLP-1 receptor agonist. Unlike injectable peptide GLP-1RAs such as semaglutide and liraglutide, orforglipron is a synthetic small molecule that is absorbed intact from the gastrointestinal tract, enabling once-daily oral dosing without the food, water, and fasting restrictions associated with SNAC-assisted peptide absorption. Orforglipron acts as a partial agonist with biased signaling at the GLP-1 receptor, engaging a binding mode distinct from peptide ligands — it activates cAMP signaling and GLP-1R downstream pathways to drive glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, and weight loss. The non-peptide nature of orforglipron overcomes the core limitations of peptide-based GLP-1 therapies — proteolytic instability, poor oral absorption, and the injection and cold-chain burden. UPOR Biotech supplies orforglipron as a white to off-white solid, available as lyophilized/amorphous powder or crystalline solid with ≥98.0% HPLC purity for reproducible in vitro and in vivo research.
As an investigational small molecule in clinical development by Eli Lilly for type 2 diabetes, obesity, and weight maintenance, orforglipron occupies a central position in oral GLP-1 receptor agonist drug discovery and the broader shift from injectable peptides to oral small-molecule metabolic therapeutics. UPOR Biotech is a bulk supplier of research-grade orforglipron for academic laboratories, pharmaceutical R&D teams, and CROs studying GLP-1R pharmacology, biased agonism, and peptide-to-small-molecule replacement strategies. This product is provided Research Use Only (RUO) — not for human diagnostic or therapeutic use. Certifications include ISO 9001, cGMP-compliant manufacturing, and FDA facility registration. Standard packaging includes 10 mg, 50 mg, 100 mg, and 1 g quantities, each accompanied by full analytical documentation (COA, HPLC, LC-MS, and NMR data on request).
Orforglipron vs Injectable GLP-1 Peptides — Oral Small-Molecule Delivery Without Injection
When comparing orforglipron vs injectable peptide GLP-1 agonists (semaglutide, liraglutide), the defining advantage is oral small-molecule delivery without injection. Peptide GLP-1RAs require subcutaneous injection (or SNAC-assisted oral absorption with strict fasting and water requirements) and cold-chain storage due to proteolytic instability. Orforglipron, as a non-peptide small molecule, is orally bioavailable, absorbed intact from the GI tract, and dosed once daily without food or water restrictions — eliminating injection-site reactions and needle burden. It is also non-immunogenic (no anti-drug antibodies against a peptide sequence), room-temperature-stable as a solid, and amenable to scalable, cost-efficient chemical synthesis without recombinant peptide manufacturing or a cold chain. These properties make orforglipron the reference small molecule for oral GLP-1 receptor agonist development and peptide-to-small-molecule replacement programs.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Orforglipron (LY3502970) — Non-Peptide GLP-1 Receptor Agonist |
| Synonyms | Orforglipron; LY3502970 |
| CAS Number | 2673951-35-7 |
| Molecular Formula | C₄₈H₄₈F₂N₁₀O₅ |
| Molecular Weight | 882.97 g/mol |
| Compound Class | Non-peptide small molecule (oral GLP-1 receptor agonist) |
| Target Receptor | GLP-1 Receptor (GLP-1R) |
| Mechanism | GLP-1R partial agonist with biased signaling (cAMP pathway activation) |
| Key Feature | First-in-class orally bioavailable non-peptide GLP-1 receptor agonist |
| Purity (HPLC) | ≥98.0% |
| Appearance | White to off-white solid / powder |
| Form | Lyophilized / amorphous powder or crystalline solid |
| Solubility | Soluble in DMSO; limited aqueous solubility |
| Endotoxin | ≤0.5 EU/mg |
| Water Content | ≤1.0% (Karl Fischer) |
| Heavy Metals | ≤10 ppm |
| Residual Solvents | Meets ICH Q3C limits |
| Storage | -20°C, desiccated, protected from light and moisture |
| Stability | Stable at -20°C; protect from light and moisture |
| Transport | Ambient / refrigerated with desiccant, per COA |
| Grade | Research Grade (RUO) |
| Applications | Type 2 diabetes, obesity, oral GLP-1 drug discovery, GLP-1R signaling studies |
| Certifications | ISO 9001, cGMP, FDA facility registration |
| Documentation | COA, MSDS/SDS, HPLC, LC-MS; NMR and elemental analysis on request |
| Packaging | 10 mg / 50 mg / 100 mg / 1 g |
| Shelf Life | 2 years (properly stored at -20°C) |
| Handling | Protect from light; prepare DMSO stock solutions for in vitro use |
| Disclaimer | Research Use Only (RUO) — not for human diagnostic or therapeutic use |
Key Benefits — Orforglipron
First-in-Class Non-Peptide GLP-1R Agonist
Orforglipron (LY3502970) is the first-in-class non-peptide, orally bioavailable GLP-1 receptor agonist — a synthetic small molecule that activates GLP-1R without any peptide sequence. Represents a new therapeutic class for oral metabolic disease treatment and drug discovery.
First-in-ClassOral Bioavailability — No Injection Required
Absorbed intact from the gastrointestinal tract for once-daily oral dosing with no injection, no cold chain, and no food or water restrictions. Overcomes the stability, absorption, and injection barriers of peptide GLP-1RAs.
Orally BioavailableBiased Partial Agonism at GLP-1R
Acts as a partial agonist with biased signaling at the GLP-1 receptor, engaging a distinct binding mode from peptide ligands and activating cAMP-dependent pathways that drive insulin secretion and weight loss.
Biased Agonism≥98% HPLC Purity Small Molecule
Supplied as a white to off-white solid with ≥98.0% HPLC purity, fully characterized by LC-MS and NMR. Research-grade material for reproducible in vitro and in vivo pharmacology studies.
≥98% HPLCApplications
Type 2 Diabetes & Glycemic Control Research
Investigate GLP-1R-mediated glucose-dependent insulin secretion, glucagon suppression, and postprandial glycemic control in cellular and animal models of type 2 diabetes.
Obesity & Weight-Loss Research
Study GLP-1R-driven delayed gastric emptying, satiety signaling, and body-weight reduction in diet-induced obesity and metabolic disease models.
Oral GLP-1 Drug Discovery & SAR Studies
Use orforglipron as a reference scaffold for structure-activity relationship (SAR) programs targeting orally bioavailable non-peptide GLP-1R agonists.
GLP-1 Receptor Signaling & Bias Studies
Probe biased agonism, cAMP accumulation, and downstream GLP-1R signaling pathways to dissect efficacy from adverse-effect signaling.
Peptide-to-Small-Molecule Replacement Research
Benchmark oral small molecules against peptide GLP-1RAs (semaglutide, liraglutide) in peptide-to-small-molecule replacement pharmacology programs.
Pharmacokinetic & Oral Bioavailability Studies
Characterize oral absorption, GI permeability, metabolic stability, and pharmacokinetic profiles of non-peptide GLP-1RAs in preclinical models.
Frequently Asked Questions
Orforglipron (LY3502970) is a non-peptide, orally bioavailable small-molecule GLP-1 receptor agonist. It acts as a partial agonist with biased signaling at GLP-1R, activating cAMP signaling and downstream pathways to produce glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, and weight loss. Its small-molecule structure binds GLP-1R via a mode distinct from peptide ligands, which underlies its oral bioavailability and once-daily dosing profile.
Orforglipron is a non-peptide small molecule, whereas semaglutide and liraglutide are peptide-based GLP-1RAs. Peptides require injection (or SNAC-assisted oral delivery with fasting restrictions) and cold-chain storage; orforglipron is orally bioavailable, absorbed intact from the GI tract, and dosed once daily without food or water restrictions. It also engages a distinct binding mode at GLP-1R and is non-immunogenic and stable as a solid, enabling scalable chemical synthesis.
Primary applications include type 2 diabetes and glycemic control research, obesity and weight-loss research, oral GLP-1 drug discovery and SAR studies, GLP-1 receptor signaling and biased-agonism studies, peptide-to-small-molecule replacement research, and pharmacokinetic and oral bioavailability studies. It serves as a reference small molecule for oral metabolic disease therapeutics.
Store at -20°C, desiccated, protected from light and moisture. Prepare stock solutions in DMSO for in vitro work (orforglipron has limited aqueous solubility); aliquot and store DMSO stocks at -20°C to avoid freeze-thaw degradation. Allow the solid to reach room temperature before opening to prevent condensation, and handle under a dry, inert atmosphere for long-term stability.
Every lot includes a Certificate of Analysis (COA), MSDS/SDS, HPLC purity data (≥98.0%), and LC-MS characterization, with NMR and elemental analysis available on request. UPOR Biotech operates under ISO 9001, cGMP, and FDA facility registration. The product is supplied Research Use Only (RUO) — not for human diagnostic or therapeutic use.