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Research Reference · Metabolic & Weight-Loss Research

Tirzepatide

A dual GIP and GLP-1 receptor agonist peptide (LY3298176) studied in weight-loss (obesity), type 2 diabetes, sleep apnea, fatty liver and heart-failure research.

Last reviewed September 2026 9 peer-reviewed sources 3-minute read

At a glance

Tirzepatide (LY3298176) is a once-weekly peptide that activates two incretin receptors, GIP and GLP-1. It is approved as a medicine for type 2 diabetes (Mounjaro) and weight management (Zepbound), and it is one of the most-studied molecules in obesity research. Lab research focuses on its unusual “imbalanced” and “biased” signaling at the two receptors.

TypeDual GIP/GLP-1 agonist peptide
Studied forObesity, diabetes, apnea, heart
Evidence stagePhase 3 trials; approved medicine
Human dataLarge randomized trials

What it’s studied for

Weight-loss (obesity) research

Substantial, sustained weight reduction over 72 weeks in adults with obesity. 3

Human · phase 3

Type 2 diabetes

Lowered HbA1c more than semaglutide 4 and improved control as a single therapy. 5

Human · phase 3

Sleep apnea & heart failure

Reduced apnea severity in obesity-related sleep apnea 7 and heart-failure events in HFpEF with obesity. 9

Human · phase 3

Fatty liver (MASH)

More participants had MASH resolution without worsening fibrosis than with placebo. 8

Human · phase 2

Tirzepatide

From $54.99 · 10 mg · 30 mg · 60 mg

Third-party tested · batch-matched COA · research use only

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How it works

Tirzepatide is a single peptide engineered to activate both the GIP and the GLP-1 receptor. 1

Lab work shows its action is “imbalanced” — weighted toward the GIP receptor — and “biased” at the GLP-1 receptor, favouring cAMP signaling over β-arrestin recruitment and causing less receptor internalization than natural GLP-1. In islet experiments this bias appeared to enhance insulin secretion. 2

In large trials it lowered blood sugar more than semaglutide in type 2 diabetes 4 and produced substantial, sustained weight reduction over 72 weeks in adults with obesity. 3 Newer trials extend the research to obstructive sleep apnea, 7 fatty liver disease 8 and heart failure with preserved ejection fraction. 9 Reviews discuss what it reveals about the role of GIP. 6

Related research

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Frequently asked questions

What is LY3298176?
The development code for tirzepatide in its discovery paper and early clinical studies.
How is tirzepatide different from semaglutide?
Semaglutide activates only the GLP-1 receptor. Tirzepatide activates both GIP and GLP-1, and in a head-to-head trial lowered HbA1c more than semaglutide.
Is tirzepatide an approved drug?
Yes — as Mounjaro for type 2 diabetes and Zepbound for weight management. Research-grade material sold here is for laboratory research only.
What does “imbalanced” and “biased” mean for tirzepatide?
It acts more strongly at the GIP receptor than at the GLP-1 receptor, and at the GLP-1 receptor it favours cAMP signaling over β-arrestin recruitment.
What is the CAS number of tirzepatide?
2023788-19-2. Its molecular formula is C225H348N48O68 (4813 g/mol).

Identifiers

Name Tirzepatide
Development code LY3298176
Class Dual GIP and GLP-1 receptor agonist (peptide)
Molecular formula C225H348N48O68
Molecular weight 4813 g/mol
CAS number 2023788-19-2
PubChem CID 166567236
Approved medicines Mounjaro · Zepbound
Supplied as Lyophilized (freeze-dried) powder

Identifiers checked against PubChem (CID 166567236).

Research timeline

  1. 2018Discovery paper: LY3298176 from preclinical work to clinical proof of concept. 1
  2. 2020Tirzepatide shown to be an imbalanced and biased dual agonist. 2
  3. 2021Phase 3 trials: SURPASS-1 as single therapy 5 and SURPASS-2 versus semaglutide. 4
  4. 2022SURMOUNT-1 in obesity 3; review of its GIP/GLP-1 mechanism. 6
  5. 2024Trials in sleep apnea 7 and MASH with liver fibrosis. 8
  6. 2025SUMMIT trial in heart failure with preserved ejection fraction and obesity. 9

Key studies

StudyModelWhat it found
Willard 2020 2 Cell + islets Imbalanced toward the GIP receptor; biased toward cAMP at the GLP-1 receptor.
Frías 2021 4 Human · phase 3 Noninferior and superior to semaglutide for HbA1c change at 40 weeks.
Jastreboff 2022 3 Human · phase 3 Substantial, sustained weight reduction over 72 weeks in obesity.
Malhotra 2024 7 Human · phase 3 Reduced apnea-hypopnea index, body weight, hsCRP and blood pressure.
Loomba 2024 8 Human · phase 2 More MASH resolution without worsening fibrosis than placebo at 52 weeks.
Packer 2025 9 Human · phase 3 Lower risk of cardiovascular death or worsening heart failure; better health status.

Sources

  1. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept. Coskun T, et al. Mol Metab, 2018. Free full text
  2. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. Willard FS, et al. JCI Insight, 2020. Free full text
  3. Tirzepatide Once Weekly for the Treatment of Obesity. Jastreboff AM, et al. N Engl J Med, 2022. Human · phase 3
  4. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. Frías JP, et al. N Engl J Med, 2021. Human · phase 3
  5. Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial. Rosenstock J, et al. Lancet, 2021. Human · phase 3
  6. Tirzepatide, a dual GIP/GLP-1 receptor co-agonist for the treatment of type 2 diabetes with unmatched effectiveness regrading glycaemic control and body weight reduction. Nauck MA, D’Alessio DA. Cardiovasc Diabetol, 2022. Free full textReview
  7. Tirzepatide for the Treatment of Obstructive Sleep Apnea and Obesity. Malhotra A, et al. N Engl J Med, 2024. Free full textHuman · phase 3
  8. Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis. Loomba R, et al. N Engl J Med, 2024. Human · phase 2
  9. Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity. Packer M, et al. N Engl J Med, 2025. Human · phase 3
For Research Use Only. This page summarizes published scientific research for educational purposes. It is not medical advice and does not promote, recommend, or describe any human or animal use. Products referenced are sold strictly for laboratory research and are not for human consumption.

Last reviewed September 2026 by Midwest Compounds. Every source above was checked against its original publication.