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Triple Incretin and Glucagon Receptor Agonist
Retatrutide
30MG per vial
Retatrutide (LY3437943) is a 39-residue synthetic peptide built on a glucose-dependent insulinotropic polypeptide (GIP) backbone and engineered to act at three class B G protein-coupled receptors at once: the GLP-1, GIP and glucagon (GCGR) receptors. Three non-coded residues shape its behaviour — α-aminoisobutyric acid at position 2, which confers resistance to dipeptidyl peptidase-4 cleavage, α-methyl-L-leucine at position 13, and a second α-aminoisobutyric acid at position 20, reported to tune GIP receptor activity and pharmacokinetic behaviour — while a C20 fatty diacid conjugated through a linker to the lysine at position 17 mediates reversible albumin binding and slows clearance. In vitro receptor pharmacology reported by Coskun and colleagues characterises the molecule as having broadly balanced GLP-1R and GCGR activity with comparatively greater GIPR activity.
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Research use only. Supplied for in vitro laboratory research. Not a drug, supplement, cosmetic or medical device, not approved by the TGA, and not for administration to humans or animals. See our research use conditions.
Compound signature
From confirmed structure
4731g/mol
Molar mass
335atoms
Heavy atoms
Atomic composition
C221H342N46O68
- C221
- H342
- N46
- O68
Characterised targets
- GLP-1R
- GIPR
- GCGR
Sequence
Tyr-Aib-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-(αMe)Leu-Leu-Asp-Lys-Lys-Ala-Gln-Aib-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 (Aib at 2 and 20; α-methyl-Leu at 13; Lys17 acylated with a C20 fatty diacid via a linker; C-terminal serinamide)
Research applications
Research on retatrutide has concentrated on what simultaneous engagement of three separate receptor pathways does to signalling, rather than on any single axis in isolation. Its relative activity at the three receptors was established in cAMP accumulation and β-arrestin recruitment assays, and it is used in vitro alongside dual GLP-1R/GIPR agonists to compare receptor activation profiles. Work in diet-induced obese rodent models has been used to dissect the individual contributions of each arm, separating GIPR- and GLP-1R-mediated effects on calorie intake from GCGR-mediated effects on energy expenditure. Cryo-electron microscopy has resolved retatrutide bound to each of the three receptors as Gs-protein complexes, allowing structural analysis of how one peptide backbone accommodates three distinct orthosteric pockets, with receptor-specific conformations in extracellular loop 1 identified as a contributor to multi-receptor agonism.
Formulation and handling
Supplied as a lyophilised powder. The C20 fatty diacid makes retatrutide markedly surface-active, so reconstitute by running the diluent slowly down the inside wall of the vial and swirling gently — shaking drives foaming and adsorption losses at the air-liquid interface, which is the commonest cause of an inconsistent recovered concentration with acylated peptides of this class.
Intended use
Retatrutide is supplied exclusively for in vitro and non-clinical scientific research. It is not approved for human or animal therapeutic, diagnostic or medicinal use. All handling and experimentation must be carried out by trained personnel in an appropriately controlled laboratory.
Specification
- Presentation
- Vial
- Labelled strength
- 30MG
- Molecular formula
- C221H342N46O68
- Molar mass
- 4731.3 g/mol
- CAS number
- 2381089-83-2
- Molecular targets
- GLP-1R, GIPR, GCGR
- Appearance
- Lyophilised powder
- Storage
- 2–8 °C sealed, −20 °C long term
Values describe the compound as supplied. Analytical figures for the material in your vial are on that lot’s certificate, not here.
Certificates of analysis
None published yetEvery lot is tested by an independent laboratory and carries its own certificate. Match the lot number printed on your vial to the certificate — a certificate for a different lot tells you nothing about yours.
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