Retatrutide (LY3437943) – Triple Hormone Receptor Agonist Research Peptide – Buy Retatrutide Online
Retatrutide (LY3437943) – Triple GIP/GLP-1/Glucagon Receptor Agonist
Retatrutide (LY3437943) is a first-in-class, unimolecular triple hormone receptor agonist that simultaneously targets the glucose-dependent insulinotropic polypeptide (GIP) receptor, glucagon-like peptide-1 (GLP-1) receptor, and glucagon (GCG) receptor . Unlike semaglutide which solely activates GLP-1R, and tirzepatide which activates both GLP-1R and GIPR, retatrutide adds glucagon receptor agonism to drive energy expenditure through thermogenesis . Compared to corresponding endogenous hormones, retatrutide is more potent at GIPR by a factor of 8.9, and less potent at GCGR and GLP-1R by factors of 0.3 and 0.4, respectively . This research-grade peptide is strictly for laboratory investigation and not intended for human or animal use.
Key Factual Details
| Attribute | Detail |
|---|---|
| Chemical Name | L-Serinamide, L-tyrosyl-2-methylalanyl-L-glutaminylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methyl-L-leucyl-L-leucyl-L-α-aspartyl-L-lysyl-N6-[N-(19-carboxy-1-oxononadecyl)-L-γ-glutamyl-2-[2-(2-aminoethoxy)ethoxy]acetyl]-L-lysyl-L-alanyl-L-glutaminyl-2-methylalanyl-L-alanyl-L-phenylalanyl-L-isoleucyl-L-α-glutamyl-L-tyrosyl-L-leucyl-L-leucyl-L-α-glutamylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide |
| Molecular Formula | C₂₂₁H₃₄₂N₄₆O₆₈ |
| Molecular Weight | 4731.34 g/mol (4.731 kDa) |
| CAS Number | 2381089-83-2 |
| Sequence | Tyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{α-Me-Leu}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(AEEA)-Lys}-Ala-Gln-{Aib}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH₂ |
| Synonyms | LY3437943 |
| Purity | ≥98% (HPLC verified) |
| Classification | Triple hormone receptor agonist (GIPR, GLP-1R, GCGR) |
Mechanism of Action & Research Applications
Triple Receptor Agonism
Retatrutide’s unique mechanism combines three complementary pathways :
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GIP Receptor (GIPR): Enhances glucose-dependent insulin secretion and promotes satiety signaling
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GLP-1 Receptor (GLP-1R): Delays gastric emptying, increases insulin secretion, suppresses appetite
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Glucagon Receptor (GCGR): Drives energy expenditure through thermogenesis, increases fat oxidation
Structural Mechanism
Cryo-electron microscopy studies reveal that retatrutide adopts a single continuous alpha-helix that penetrates the receptor transmembrane domain via its N-terminal segment (residues 1–13), while its C-terminal segment interacts with the extracellular domain . The triple agonism is achieved through a combination of common interactions with conserved residues (including salt bridges with E⁶·⁵³ᵇ and E/D⁷·⁴²ᵇ, stacking interactions with tryptophan residues, and hydrogen bonding networks) and receptor-specific contacts that accommodate structural variations in each receptor .
Research Applications:
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Metabolic Research: Investigating multi-target incretin pathways for obesity and type 2 diabetes
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Energy Expenditure Studies: Examining GCGR-mediated thermogenesis mechanisms
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Cardiovascular-Kidney-Metabolic (CKM) Research: Exploring systemic hemodynamic effects
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Hepatic Steatosis Models: Investigating liver fat reduction pathways
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Receptor Interaction Studies: Characterizing GIPR, GLP-1R, and GCGR binding dynamics
Research Parameters
All dosages are for in-vitro and preclinical research use only and are not intended for human consumption.
Clinical Research Dosing (Phase 2 Data) :
| Dose | Weight Loss at 24 Weeks | Weight Loss at 48 Weeks |
|---|---|---|
| 4 mg (once weekly) | ~15.2% fat mass reduction | Not reported |
| 8 mg (once weekly) | ~26.1% fat mass reduction | Not reported |
| 12 mg (once weekly) | ~17.5% total body weight | 24.2% total body weight |
Key Clinical Observations :
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63% of participants achieved ≥20% total body weight loss at 12 mg dose
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23.2% reduction in fat mass confirmed by DXA (dual-energy X-ray absorptiometry) scans
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Absolute HbA1c reduction of 2.02% in type 2 diabetes patients
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27% of diabetic participants reached normoglycemia (HbA1c < 5.7%)
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82.4% relative reduction in hepatic fat; normalization in 86% of patients
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Systolic blood pressure reduction: 8.79 mm Hg
Storage:
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Store lyophilized powder at -20°C
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Protect from light and moisture
Order Retatrutide Today – Request a quote for your metabolic research project. Available in various pack sizes with COA. Contact our sales team for bulk pricing and custom synthesis inquiries.











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