Orforglipron
Also known as: LY3502970 · Oral GLP-1 agonist · Orfor
The first truly oral (tablet) GLP-1 receptor agonist that is a small molecule — not a peptide requiring oral protection like semaglutide (Rybelsus). Phase 3 trials showed 14.7% weight loss, close to injectable semaglutide. No needle required — once-daily pill with no food restrictions.
Mechanism of Action
Unlike oral semaglutide (which still requires fasting and is poorly absorbed), Orforglipron is a small non-peptide molecule that binds the GLP-1 receptor with high affinity regardless of food. It activates the same GLP-1 signaling pathways as injectable GLP-1 agonists but with convenient once-daily oral administration and no formulation restrictions.
Benefits
- Fully oral — no injections required
- Phase 3: 14.7% weight loss (comparable to injectable semaglutide)
- No food restrictions for absorption (unlike Rybelsus)
- Once-daily pill convenience
- Significant HbA1c reduction for type 2 diabetes
- Manufacturing cost advantages over peptide injectables
Side Effects & Risks
- Nausea and vomiting (GLP-1 class)
- GI side effects similar to injectable GLP-1s
- Phase 3 trials ongoing — not yet FDA approved
- Small molecule — not technically a peptide
Where to Buy Orforglipron
2 options across 2 vendors · Sorted cheapest first · All include direct product link
From
$249.99
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Storage & Reconstitution Guide
Storage Temperature
-20°C (lyophilized)
24 months (lyophilized), 28 days (reconstituted)
Reconstitution Solvent
Bacteriostatic water (BAC water)
Swirl gently — do not shake or vortex
Handling Notes
Protect lyophilized peptide from moisture and light. Once reconstituted, keep refrigerated. Discard if solution becomes cloudy or discolored. Use insulin syringe for precise dosing.
Step-by-Step Reconstitution
Gather supplies
BAC water, insulin syringe, alcohol swabs, vial
Disinfect tops
Swab rubber stoppers of both vials with alcohol
Draw BAC water
Pull desired mL of BAC water into syringe
Inject slowly
Inject BAC water down the side of the peptide vial, swirl gently to dissolve
Research Protocol
- Dose Range
- 12–36 mg
- Frequency
- Once daily oral
- Cycle
- Ongoing / chronic
- Routes
- oral
- Notes
- Phase 3 doses: 12-45mg/day. Starting dose 12mg/day, titrate up. FDA approval expected 2025-2026. Available from some research vendors as capsules.
Legal & Regulatory Status
Sold for research purposes only. Not for human use. Laws vary by country.
Commonly Stacked With
View all peptide stacks →External Resources
Chemical Properties
- CAS Number
- 2187743-93-3
- Mol. Weight
- C24H26F3N3O3S
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