Compound monograph
Retatrutide
Retatrutide, development code LY3437943, is a single peptide characterized as an agonist at GCGR, GIPR, and GLP-1R in its discovery record.
01
Identity & nomenclature
Retatrutide, development code LY3437943, is a single peptide characterized as an agonist at GCGR, GIPR, and GLP-1R in its discovery record.
Retatrutide is the adopted name used for the development compound LY3437943 in the verified bibliography.
Declared aliases and development codes: LY3437943.
02
Molecular properties
| CAS Registry Number | 2381089-83-2 |
|---|---|
| UNII | NOP2Y096GV |
03
Structural characteristics
Like tirzepatide, retatrutide is built on a GIP scaffold rather than a GLP-1 scaffold, with a different substitution set, lipidation position and spacer. The related GIP(1-42) entry identifies scaffold ancestry; GLP-1(7-36) amide and glucagon are native receptor comparators. Activity at the GLP-1 and glucagon receptors is engineered pharmacology and does not make retatrutide a GLP-1-derived or glucagon-derived peptide. Tirzepatide's modification table does not apply to it. No residue-by-residue substitution list is stated because this entry has no recorded sequence or molecular formula against which to verify one. Formula, mass, and sequence remain unpopulated because no authoritative public record for them was verified. The CAS registry number and UNII are recorded from the FDA/NCATS GSRS substance record, which lists both as primary on the retatrutide entry. No PubChem CID is published here: PubChem holds this compound as a substance record rather than a compound record, so there is no CID to cite.
04
Molecular targets & mechanisms
Glucagon-like peptide-1 receptor
GLP-1R
GLP-1R is a class B G-protein-coupled receptor. The cited structural and pharmacology records characterize semaglutide and retatrutide as peptide agonists at this receptor.
Glucose-dependent insulinotropic polypeptide receptor
GIPR
GIPR is a class B G-protein-coupled receptor. The cited discovery and trial records identify it as one of the three receptor relationships declared for retatrutide.
Glucagon receptor
GCGR
GCGR is a class B G-protein-coupled receptor. Retatrutide's LY3437943 discovery record characterizes a molecular agonist relationship at GCGR alongside GIPR and GLP-1R.
05
Analytical considerations
Analytical identity values are intentionally not inferred from catalog copy or from structurally related peptides.
06
Verified bibliography
- LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept.current
Coskun T, Urva S, Roell WC, Qu H, Loghin C, Moyers JS, O'Farrell LS, Briere DA, Sloop KW, Thomas MK, Pirro V, Wainscott DB, Willard FS, Abernathy M, Morford L, Du Y, Benson C, Gimeno RE, Haupt A, Milicevic Z
Cell metabolism · 2022-08-18 · Journal Article
- Triple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial.current
Jastreboff AM, Kaplan LM, Frías JP, Wu Q, Du Y, Gurbuz S, Coskun T, Haupt A, Milicevic Z, Hartman ML, Retatrutide Phase 2 Obesity Trial Investigators
The New England journal of medicine · 2023-06-26 · Clinical Trial, Phase II
- Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA.current
Rosenstock J, Frias J, Jastreboff AM, Du Y, Lou J, Gurbuz S, Thomas MK, Hartman ML, Haupt A, Milicevic Z, Coskun T
Lancet (London, England) · 2023-06-26 · Clinical Trial, Phase II
- Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial.current
Sanyal AJ, Kaplan LM, Frias JP, Brouwers B, Wu Q, Thomas MK, Harris C, Schloot NC, Du Y, Mather KJ, Haupt A, Hartman ML
Nature medicine · 2024-06-10 · Clinical Trial, Phase II
- Pharmacology, physiology, and mechanisms of incretin hormone action.current
Campbell JE, Drucker DJ
Cell metabolism · 2013-05-16 · Review
- Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein.current
Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G
Nature · 2017-05-24 · Journal Article
- Structural basis for ligand recognition of incretin receptors.current
Underwood CR, Parthier C, Reedtz-Runge S
Vitamins and hormones · 2010 · Review
- Structure of the full-length glucagon class B G-protein-coupled receptor.current
Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B
Nature · 2017-05-17 · Journal Article
- Structure of the glucagon receptor in complex with a glucagon analogue.current
Zhang H, Qiao A, Yang L, Van Eps N, Frederiksen KS, Yang D, Dai A, Cai X, Zhang H, Yi C, Cao C, He L, Yang H, Lau J, Ernst OP, Hanson MA, Stevens RC, Wang MW, Reedtz-Runge S, Jiang H, Zhao Q, Wu B
Nature · 2018-01-03 · Journal Article
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Methodology & citation verification
Reference identity is checked against official PubMed metadata. Local deterministic receipts bind each normalized title and canonical metadata record to its verification date. Scientific values remain absent when an authoritative source has not been verified.
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