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Tirzepatide

Mounjaro · Zepbound · LY3298176

Metabolic & WeightApproved
From$5.15/mgCompare prices
MW
4813g/mol
Formula
C225H348N48O68

Tirzepatide is a novel peptide classified as a dual agonist of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, originally developed for the management of obesity and metabolic disorders. Researchers primarily study tirzepatide for its potential effects on weight reduction and its implications for related conditions such as type 2 diabetes and cardiovascular health. Key findings from recent studies indicate that tirzepatide can lead to significant reductions in body weight and improvements in metabolic parameters, with participants experiencing an average weight loss of up to 20% over 72 weeks, as well as a lower risk of developing type 2 diabetes compared to placebo. Additionally, evidence suggests that tirzepatide may reduce the severity of obstructive sleep apnea and improve cardiovascular outcomes in patients with obesity. Current research continues to explore its long-term safety and efficacy across various populations and health conditions.

Chemical Profile

Chemical Profile

Chemical structure
Chemical Structure
FormulaC225H348N48O68
Molecular Weight4813 g/mol
CAS Number2023788-19-2
PubChem CID166567236

Half-Life

SCSubcutaneous

~5 days

IVIntravenous

Not applicable

INIntranasal

Not applicable

POOral

Poor bioavailability

The long half-life supports once-weekly dosing for subcutaneous administration.

Mechanism

Mechanism of Action

Tirzepatide is a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor, activating signaling pathways that enhance insulin secretion, suppress glucagon release, and promote satiety through the cAMP/PKA and PI3K/Akt pathways. This results in reduced appetite, increased energy expenditure, and significant weight loss, along with improvements in metabolic parameters such as blood glucose levels and cardiovascular outcomes. While the precise mechanisms underlying its effects on weight loss and metabolic health are still being elucidated, the activation of these receptors plays a crucial role in mediating its therapeutic effects.

Research

64 Research Publications

14,944

Total Citations

34

Human/RCT

21.9

Avg. Influence

2025

Latest

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#01

Tirzepatide Once Weekly for the Treatment of Obesity.

HumanInfluence348.0
2502
The study demonstrated that once-weekly tirzepatide resulted in substantial and sustained weight loss in humans with obesity over 72 weeks compared to placebo.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#02

Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes.

Frías Juan P, et al. · The New England journal of medicine · 2021

HumanInfluence114.0
1295
Researchers observed that tirzepatide was noninferior and superior to semaglutide in reducing glycated hemoglobin levels and body weight in humans with type 2 diabetes over 40 weeks.

Key findings

  1. 01Tirzepatide significantly reduced blood sugar levels more than semaglutide.
  2. 02Participants taking tirzepatide experienced greater weight loss compared to those on semaglutide.
  3. 03The most common side effects for both medications were mild to moderate gastrointestinal issues.
2.4 mgsubcutaneously(human)68 weeks2.4 mgsubcutaneously(human)68 weeks5 mgsubcutaneously(human)40 weeks10 mgsubcutaneously(human)40 weeks15 mgsubcutaneously(human)40 weeks1 mgsubcutaneously(human)40 weeks14 mgoral(human)not mentioned0.5 mgsubcutaneously(human)30 weeks1.0 mgsubcutaneously(human)30 weeks2.4 mgsubcutaneously(human)32 weeks2.4 mgsubcutaneously(human)32 weeks1.0 mgsubcutaneously(human)56 weeks2.0 mgsubcutaneously(human)56 weeks
PubMed
#03

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 Julio, et al. · Lancet (London, England) · 2021

HumanInfluence68.0
670
Researchers observed that tirzepatide significantly improved glycemic control and body weight in humans with type 2 diabetes compared to placebo without increasing the risk of hypoglycemia.

Key findings

  1. 01Tirzepatide led to significant improvements in blood sugar control compared to a placebo.
  2. 02Participants experienced notable weight loss while using tirzepatide.
  3. 03The safety profile of tirzepatide was similar to existing GLP-1 receptor agonists, suggesting it could be a viable treatment option.
10 or 15 mgsubcutaneous(human)36 weeks5 mgsubcutaneous(human)176 weeks5 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks5 mgsubcutaneous(human)52 weeks10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks
PubMed
#04

Continued Treatment With Tirzepatide for Maintenance of Weight Reduction in Adults With Obesity: The SURMOUNT-4 Randomized Clinical Trial.

Aronne Louis J, et al. · JAMA · 2024

HumanInfluence49.0
668
Researchers observed that continued treatment with tirzepatide significantly maintained weight loss compared to placebo in adults with obesity, while withdrawal led to substantial weight regain.

Key findings

  1. 01Participants who continued tirzepatide maintained an average weight loss of 25.3% over 88 weeks, compared to 9.9% for those on placebo.
  2. 0289.5% of participants on tirzepatide maintained at least 80% of their weight loss, while only 16.6% of those on placebo did.
  3. 03The most common side effects were mild to moderate gastrointestinal issues, more frequent in the tirzepatide group.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#05

Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis.

Loomba Rohit, et al. · The New England journal of medicine · 2024

HumanInfluence47.0
614
Researchers observed that tirzepatide was more effective than placebo in resolving metabolic dysfunction-associated steatohepatitis without worsening fibrosis in humans after 52 weeks.

Key findings

  1. 0144% of participants taking 5 mg of tirzepatide saw resolution of MASH without worsening fibrosis, compared to 10% in the placebo group.
  2. 0262% of participants taking 15 mg of tirzepatide achieved the same resolution, showing a significant benefit over placebo.
  3. 03The most common side effects reported were mild to moderate gastrointestinal issues.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#06

Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity.

HumanInfluence47.0
602
The study demonstrated that treatment with tirzepatide reduced the risk of cardiovascular events and improved health status in humans with heart failure and obesity compared to placebo.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#07

Obesity Management in Adults: A Review.

ReviewInfluence27.0
595
The study demonstrated that comprehensive obesity management strategies, including medications like tirzepatide, can lead to significant weight loss and improved health outcomes in adults.
2.4 mgsubcutaneously(human)68 weeks2.4 mgsubcutaneously(human)68 weeks5 mgsubcutaneously(human)40 weeks10 mgsubcutaneously(human)40 weeks15 mgsubcutaneously(human)40 weeks1 mgsubcutaneously(human)40 weeks14 mgoral(human)not mentioned0.5 mgsubcutaneously(human)30 weeks1.0 mgsubcutaneously(human)30 weeks2.4 mgsubcutaneously(human)32 weeks2.4 mgsubcutaneously(human)32 weeks1.0 mgsubcutaneously(human)56 weeks2.0 mgsubcutaneously(human)56 weeks
PubMed
#08

Tirzepatide once weekly for the treatment of obesity in people with type 2 diabetes (SURMOUNT-2): a double-blind, randomised, multicentre, placebo-controlled, phase 3 trial.

HumanInfluence57.0
522
The study demonstrated that tirzepatide significantly reduced body weight in humans with obesity and type 2 diabetes compared to placebo over 72 weeks.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#09

Effect of Subcutaneous Tirzepatide vs Placebo Added to Titrated Insulin Glargine on Glycemic Control in Patients With Type 2 Diabetes: The SURPASS-5 Randomized Clinical Trial.

Dahl Dominik, et al. · JAMA · 2022

HumanInfluence35.0
505
Researchers observed that adding tirzepatide to insulin glargine significantly improved glycemic control and reduced body weight in patients with type 2 diabetes compared to placebo.

Key findings

  1. 01Participants using tirzepatide had an average decrease in blood sugar levels of up to 2.4% compared to 0.9% in the placebo group.
  2. 02Those treated with tirzepatide lost between 5.4 kg and 8.8 kg, while the placebo group gained 1.6 kg.
  3. 03A higher percentage of patients on tirzepatide achieved target blood sugar levels of less than 7% compared to those on placebo.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
#10

Tirzepatide for the Treatment of Obstructive Sleep Apnea and Obesity.

HumanInfluence47.0
492
Researchers observed that tirzepatide significantly reduced the apnea-hypopnea index and body weight in humans with moderate-to-severe obstructive sleep apnea and obesity compared to placebo.
10 mgsubcutaneous(human)52 weeks15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)176 weeksup to 15 mgsubcutaneous(human)52 weeks5 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)40 weeks15 mgsubcutaneous(human)40 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks10 mgsubcutaneous(human)72 weeks15 mgsubcutaneous(human)72 weeks
PubMed
Safety

Safety & Handling

Research Gaps

The long-term effects of tirzepatide beyond three years of treatment in diverse populations, particularly those with varying comorbidities, remain unclear. Additionally, the specific mechanisms by which tirzepatide influences cardiovascular outcomes and its comparative efficacy against other obesity treatments in individuals without type 2 diabetes have not been fully elucidated.

Solubility

Tirzepatide is soluble in water and exhibits limited solubility in organic solvents such as acetonitrile and DMSO.

Storage & Handling

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Approved by the FDA for the treatment of type 2 diabetes. Not a controlled substance.

🇦🇺AU

Approved by the TGA for the treatment of type 2 diabetes.

🇬🇧UK

Approved by the MHRA for the treatment of type 2 diabetes.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Community Insights

Community Insights

Publications per Year

50 total
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Pricing

Price Comparison

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  • Polaris PeptidesUS
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    $11.00/mg

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer