Dual GIP/GLP-1 Receptor Agonist / Twincretin
Tirzepatide Research Compound — Dual GIP/GLP-1 Receptor Agonist
Tirzepatide (LY3298176) is a 39-amino acid synthetic peptide that functions as a dual agonist of both the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R) — a pharmacological profile designated a 'twincretin.' It was developed by Eli Lilly as the first approved dual incretin receptor agonist and is used in metabolic research to study combined GIPR/GLP-1R axis activation.
Compound identity
- Name
- Tirzepatide
- Class
- Dual GIP/GLP-1 Receptor Agonist / Twincretin
- CAS number
- 2023788-19-2
- Molecular formula
- C₂₂₅H₃₄₈N₄₈O₆₈
- Also known as
- GIP/GLP-1 dual agonist, LY3298176, Mounjaro peptide
- Sequence
- 39-aa dual GIP/GLP-1R agonist; GIP agonist scaffold (positions 1-15) + modified amino acids; C20 fatty diacid conjugated via linker to Lys20 (albumin binding); MW 4813.47 Da
Research context
Tirzepatide (CAS 2023788-19-2, MW 4813.47 Da, C₂₂₅H₃₄₈N₄₈O₆₈) is a 39-amino acid peptide built on a modified GIP(1-15) agonist scaffold with additional structural elements that confer GLP-1R co-agonism. The compound incorporates multiple non-natural amino acids including Aib substitutions at several positions for DPP-4 resistance, and a C20 fatty diacid conjugated via a γGlu-miniPEG linker to Lys20 for albumin binding — extending the half-life to approximately 5 days in humans. Unlike GLP-1R monoagonists (semaglutide, liraglutide), tirzepatide achieves balanced agonism at both GIPR and GLP-1R. GIP (glucose-dependent insulinotropic polypeptide) is the other major incretin hormone, secreted from intestinal K cells in response to fat and carbohydrate ingestion; it potentiates insulin secretion and has additional roles in adipose tissue lipid storage, bone metabolism, and CNS energy balance signaling.
The research rationale for dual GIPR/GLP-1R agonism emerged from the paradoxical finding that GIPR-knockout mice are protected from obesity when fed a high-fat diet, while separately, GIPR antagonism combined with GLP-1R agonism produced additive weight loss in rodent models. The GIPR/GLP-1R co-agonism approach in tirzepatide was developed to leverage complementary mechanisms: GLP-1R agonism reduces appetite and slows gastric emptying; GIPR agonism in adipose tissue (GIPR is expressed on adipocytes) may enhance lipid metabolism and GLP-1R sensitization. SURPASS clinical trial program data with tirzepatide demonstrated superior HbA1c and body weight reductions compared to GLP-1R monoagonism, supporting the mechanistic hypothesis. Research using tirzepatide as a dual receptor probe has examined GIPR/GLP-1R synergy in β-cell insulin secretion, adipocyte biology, hepatic lipid metabolism, and CNS appetite regulation.
As a research reagent, tirzepatide is used in studies of dual incretin receptor pharmacology, GIPR and GLP-1R cross-talk, metabolic disease models, obesity biology, adipocyte lipid metabolism, and β-cell function. DMV Research supplies tirzepatide as a lyophilized compound with per-batch Certificate of Analysis confirming identity by mass spectrometry and purity ≥99% by HPLC.
Frequently asked questions
What is tirzepatide?+
Tirzepatide (CAS 2023788-19-2, LY3298176) is a 39-amino acid dual agonist of the GIP receptor (GIPR) and GLP-1 receptor (GLP-1R), developed by Eli Lilly. Its 'twincretin' profile — activating both major incretin receptors — distinguishes it from GLP-1R monoagonists like semaglutide. It is the active ingredient in Mounjaro (type 2 diabetes) and Zepbound (obesity). As a research compound, tirzepatide is used in metabolic biology to probe dual GIPR/GLP-1R signaling, adipocyte biology, β-cell function, and obesity models.
How does tirzepatide differ from semaglutide?+
Semaglutide is a GLP-1R monoagonist (acts only at GLP-1R). Tirzepatide is a dual GIPR/GLP-1R agonist — it activates both the GIP receptor and the GLP-1 receptor. GIPR is expressed on β-cells (potentiates insulin secretion), adipocytes (lipid metabolism), bone cells, and CNS neurons. The additional GIPR agonism contributes to tirzepatide's mechanism and distinct pharmacological profile compared to GLP-1R monoagonism alone. In clinical research, tirzepatide demonstrated greater HbA1c lowering and weight loss than semaglutide at comparable doses in the SURPASS-2 trial.
What is the GIPR (GIP receptor) and why does dual agonism matter in research?+
GIP (glucose-dependent insulinotropic polypeptide, also called gastric inhibitory polypeptide) is a 42-aa incretin hormone secreted from intestinal K cells in response to nutrient ingestion. GIPR, the GIP receptor, is expressed on pancreatic β-cells, adipocytes, osteoblasts, and CNS neurons. Like GLP-1R, GIPR is a class B GPCR signaling primarily through cAMP. Dual GIPR/GLP-1R agonism is studied in research because it provides a tool to examine whether incretin receptor co-activation synergizes, is additive, or involves cross-sensitization — questions relevant to understanding metabolic disease biology and therapeutic mechanism.
Is tirzepatide a research-only compound at DMV Research?+
Yes. As supplied by DMV Research, tirzepatide is a research compound for in-vitro and pre-clinical laboratory research use only — not for human consumption. Tirzepatide is the active pharmaceutical ingredient in FDA-approved prescription medications (Mounjaro, Zepbound) that require a valid prescription and are dispensed through licensed pharmacies. DMV Research supplies research-grade tirzepatide solely for laboratory research purposes.
Research use only
All products are intended for laboratory and research use only (RUO) and are not for human consumption, ingestion, or any in-vivo use.
The statements on this page have not been evaluated by the FDA. Tirzepatide is not intended to diagnose, treat, cure, or prevent any disease. Content is provided for laboratory research reference only.