Retatrutide (LY3437943) Research Grade Peptide (Triple Agonist) Supplier — UPOR Biotech
Retatrutide (LY3437943) is a synthetic 39-residue peptide engineered as a unimolecular triple agonist of GIPR, GLP-1R, and the glucagon receptor (GCGR) — the first-in-class molecule targeting all three metabolic receptor systems at once. This GIPR-biased triple agonism drives glucose-dependent insulin secretion, glucagon-mediated energy expenditure, and up to ~45% weight loss in obese-mouse models, making it a defining tool for obesity and type 2 diabetes research. Research Grade (RUO) retatrutide peptide with a once-weekly dosing design — from UPOR Biotech.
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Retatrutide (LY3437943, CAS 2381089-83-2, C₂₂₁H₃₄₂N₄₆O₆₈, MW 4731.33 g/mol) is a synthetic 39-residue peptide engineered as a unimolecular triple agonist of the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). The sequence incorporates non-native Aib and α-Me-Leu residues for enhanced metabolic stability and carries a C20 fatty-diacid C-terminal linker for prolonged pharmacokinetics. Retatrutide exhibits a GIPR-biased potency profile in human receptor assays — GIPR EC50 0.0643 nM, GLP-1R EC50 0.775 nM, GCGR EC50 5.79 nM. Simultaneous GIP/GLP-1/glucagon signaling produces glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, reduced food intake, and increased energy expenditure. In obese-mouse studies, retatrutide achieved weight loss up to ~45%, with GCGR agonism contributing an estimated ~30–35% of the effect — the basis of its differentiation from dual-agonist peptides.
Retatrutide is positioned at the leading edge of obesity and type 2 diabetes (T2D) research, representing a triple-agonist evolution beyond dual GIP/GLP-1 agents like tirzepatide. Its once-weekly pharmacokinetic profile — conferred by the C20 diacid linker — supports chronic-dosing study designs and pharmacodynamic evaluation of long-acting incretin/glucagon combination signaling. Research Use Only (RUO) — not for human diagnostic or therapeutic use. Every lot is characterized by HPLC (≥98.0% purity), mass spectrometry, and endotoxin analysis, with a full Certificate of Analysis. Supplied lyophilized under ISO 9001:2015 and cGMP-compliant production at an FDA-registered facility, packaged in 1 / 5 / 10 / 50 mg vials for research laboratories, biotech, and CRO applications.
Retatrutide vs Tirzepatide — Triple Agonist vs Dual GIP/GLP-1 Agonist
When comparing retatrutide vs tirzepatide, the defining difference is that retatrutide adds glucagon receptor (GCGR) agonism to the dual GIP/GLP-1 platform of tirzepatide. Both molecules are once-weekly, fatty-acid-linked incretin agonists, but the third receptor arm changes the pharmacology: GCGR activation drives greater energy expenditure and thermogenesis, which is why retatrutide produces more pronounced weight loss in research models (up to ~45% in obese mice vs ~20-25% for tirzepatide). Retatrutide retains a GIPR-biased potency profile — GIPR EC50 0.0643 nM vs GLP-1R 0.775 nM vs GCGR 5.79 nM — mirroring the GIP-preferring design of tirzepatide while layering on glucagon-mediated metabolic benefit. For researchers modeling the next generation of metabolic receptor co-agonism, retatrutide is the reference triple agonist for obesity and T2D mechanism studies.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Retatrutide (LY3437943) — Research Grade (RUO) |
| Synonyms | Retatrutide; LY3437943 |
| CAS Number | 2381089-83-2 |
| Molecular Formula | C₂₂₁H₃₄₂N₄₆O₆₈ (free acid) |
| Molecular Weight | 4731.33 g/mol |
| Amino Acid Length | 39 residues |
| Salt Form | Free acid / TFA salt as supplied |
| Peptide Class | Triple incretin/glucagon receptor agonist (GIPR / GLP-1R / GCGR) |
| Structural Features | Non-native Aib and α-Me-Leu residues; C20 fatty-diacid C-terminal linker for prolonged pharmacokinetics |
| Mechanism | Simultaneous GCGR/GIPR/GLP-1R agonism — glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, reduced food intake, increased energy expenditure |
| Receptor Target | Glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon-like peptide-1 receptor (GLP-1R) |
| Potency (Human EC50) | GIPR 0.0643 nM; GLP-1R 0.775 nM; GCGR 5.79 nM |
| Receptor Selectivity | GIPR-biased triple agonism |
| Purity (HPLC) | ≥98.0% |
| Appearance | White to off-white lyophilized powder |
| Solubility | Soluble in sterile water, dilute PBS (pH 7.4), and 0.1 M acetic acid; reconstitute with gentle swirling, avoid vigorous vortexing |
| Endotoxin | ≤1.0 EU/mg |
| Water Content | ≤5.0% |
| Heavy Metals | ≤10 ppm |
| Storage | -20°C, lyophilized, protected from light and moisture, desiccated |
| Stability | Stable lyophilized at -20°C; aliquot reconstituted peptide and avoid repeated freeze-thaw cycles |
| Grade | Research Grade (RUO) |
| Applications | Obesity & weight-loss research, type 2 diabetes (T2D) studies, metabolic & energy-expenditure pharmacology, incretin receptor co-agonism research, once-weekly dosing PK, peptide reference standards & assay development |
| Certifications | ISO 9001:2015, cGMP-compliant production, FDA facility registration |
| Packaging | 1 / 5 / 10 / 50 mg sealed vials |
| Shelf Life | 2 years (lyophilized, -20°C) |
| Disclaimer | Research Use Only (RUO) — not for human diagnostic or therapeutic use |
Key Benefits — Retatrutide (LY3437943)
Unimolecular Triple Receptor Agonism
A single 39-residue peptide activates GCGR, GIPR, and GLP-1R simultaneously — the first triple-agonist architecture targeting glucagon, incretin, and insulinotropic signaling in one molecule. Built on Aib/α-Me-Leu-stabilized sequence with a C20 fatty-diacid linker for sustained action.
Triple AgonistGIPR-Biased Potency Profile (EC50 0.0643 nM)
Highest potency at the GIP receptor (EC50 0.0643 nM), with balanced GLP-1R (0.775 nM) and GCGR (5.79 nM) activity — a GIPR-biased design that mirrors the pharmacological strategy validated by dual-agonist incretin platforms while adding a third arm.
GIPR EC50 0.0643 nMGlucagon-Mediated Energy Expenditure
GCGR agonism drives energy expenditure and thermogenesis, contributing an estimated ~30–35% of the up to ~45% weight loss observed in obese-mouse models — the mechanism that differentiates triple from dual agonists in metabolic research.
GCGR Mechanism≥98% HPLC Purity Research Peptide
≥98.0% HPLC purity with full characterization — mass spectrometry, endotoxin ≤1.0 EU/mg, water content ≤5.0% — documented in a complete COA. Research Grade (RUO), supplied lyophilized under ISO 9001:2015 / cGMP / FDA-registered production.
≥98% HPLCApplications
Obesity & Weight-Loss Research
Dose-response and chronic-dosing studies of body-weight reduction, food intake, and fat-mass loss using the reference triple-agonist molecule (up to ~45% weight loss in obese-mouse models).
Type 2 Diabetes (T2D) Studies
Investigation of glucose-dependent insulin secretion, glucagon suppression, and glycemic control in T2D and metabolic-disease models.
Metabolic & Energy-Expenditure Pharmacology
Quantification of thermogenesis, energy balance, and GCGR-mediated expenditure pathways in metabolic phenotyping platforms.
Incretin Receptor Co-Agonism Research
Mechanistic dissection of GIPR / GLP-1R / GCGR signaling crosstalk in receptor-binding, signaling-bias, and functional-cell assays.
Once-Weekly Dosing Pharmacokinetics
PK/PD evaluation of the C20 fatty-diacid-linked long-acting design, including half-life, exposure, and sustained-receptor-occupancy profiling.
Peptide Reference Standard & Assay Development
Use as an analytical reference standard in HPLC, LC-MS, and cell-based potency assays for metabolic-receptor-agonist discovery programs.
Frequently Asked Questions
Retatrutide (LY3437943) is a synthetic 39-residue peptide engineered as a unimolecular triple agonist of the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). It carries a C20 fatty-diacid C-terminal linker conferring a once-weekly pharmacokinetic profile. Simultaneous GIP/GLP-1/glucagon signaling drives glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, reduced food intake, and increased energy expenditure. In obese-mouse studies, retatrutide produced weight loss up to ~45%, with GCGR activation contributing roughly 30–35% of the total effect.
Tirzepatide is a dual GIP/GLP-1 receptor agonist. Retatrutide builds on that same GIP/GLP-1 platform and adds a third component — glucagon receptor (GCGR) agonism — making it a triple agonist. This additional GCGR activity drives greater glucagon-mediated energy expenditure and thermogenesis in research models, the basis of the larger weight loss (up to ~45%) observed with retatrutide versus ~20-25% reported with tirzepatide. The GIPR-biased potency profile (GIPR EC50 0.0643 nM vs GLP-1R 0.775 nM vs GCGR 5.79 nM) further distinguishes the two molecules at the receptor level.
Retatrutide is used primarily in obesity and weight-loss research, type 2 diabetes (T2D) studies, and metabolic pharmacology. Its triple agonism makes it a valuable tool for investigating incretin and glucagon receptor co-signaling, energy-expenditure regulation, and once-weekly dosing pharmacokinetics. It is also used as a peptide reference standard and in receptor-binding and functional-cell assay development targeting GIPR, GLP-1R, and GCGR.
Store lyophilized retatrutide at -20°C, protected from light and moisture, and keep desiccated. Reconstitute in sterile water for injection, dilute phosphate-buffered saline (PBS), or 0.1 M acetic acid to the desired concentration. Avoid vigorous vortexing — gentle swirling minimizes foaming and aggregation. Once reconstituted, avoid repeated freeze-thaw cycles; aliquot and store at -20°C for long-term use or 2-8°C for short-term use. Handle in a controlled research environment only.
Every shipment includes a Certificate of Analysis (COA) confirming ≥98.0% HPLC purity, MSDS, HPLC chromatogram, mass spectrometry (MS) analysis, and endotoxin (≤1.0 EU/mg) and water-content results. UPOR Biotech operates under ISO 9001:2015 quality management, cGMP-compliant production, and FDA facility registration. This product is Research Grade (RUO) — Research Use Only — and is not for human diagnostic or therapeutic use. Full lot traceability is provided with every order.