Peptides > Tirzepatide


Tirzepatide is a synthetic compound derived from gastric inhibitory polypeptide (GIP), and it possesses the simultaneous functionality of glucagon-like peptide-1 (GLP-1). This unique combination enables Tirzepatide to have multiple beneficial effects, including lowering blood glucose levels, enhancing insulin sensitivity, promoting feelings of fullness, and facilitating weight loss. Initially developed to combat type 2 diabetes, Tirzepatide has also demonstrated its ability to protect the cardiovascular system and act as a powerful agent for weight loss.

This PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. All product information available on this website is for educational purposes only. Bodily introduction of any kind into humans or animals is strictly forbidden by law. This product should only be handled by licensed, qualified professionals. This product is not a drug, food, or cosmetic and may not be misbranded, misused or mislabled as a drug, food or cosmetic.


1. Tirzepatide


2. Tirzepatide Structure


3. What Does Tirzepatide Do?


Tirzepatide is a synthetic analog of gastric inhibitory polypeptide (GIP) developed for its capacity to stimulate insulin release, addressing both type 2 diabetes and non-alcoholic fatty liver disease. Comprising 39 amino acids, Tirzepatide, despite its relatively large size, stimulates insulin release from the pancreas by binding to both GIP and GLP-1 (glucagon-like peptide-1) receptors. Over extended periods of use, Tirzepatide can increase adiponectin levels by up to 26%[1]. Research indicates that Tirzepatide reduces feelings of hunger, decreases insulin levels, and enhances insulin sensitivity. Collectively, these effects result in significant weight loss of approximately 11 kg (25 lbs), improved glucose tolerance, reduced adipose tissue, and a decreased cardiovascular risk.

Tirzepatide Structure

Amino Acid Sequence: YE-Aib-GTFTSDYSI-Aib-LDKIAQ (C20 fatty acid) AFVQWLIAGGPSSGAPPPS
  Note: Aib is a non-coded (non-proteinogenic) amino acid – H2H-C(CH3)2COOH
Molecular Formula: C225H348N48O68
Molecular Weight:
 4813.527 g/mol
PubChem CID: 156588324
CAS Number: 2023788-19-2
Synonyms: P1206, LY3298176

What Does Tirzepatide Do?

Tirzepatide is a peptide that has shown promise in the treatment of Type 2 diabetes. It works by increasing the release of insulin from the pancreas, leading to improved glucose control. Research has indicated that Tirzepatide can significantly reduce hemoglobin A1c (HbA1c) levels, a marker of long-term blood sugar control, by 2.4% after six months of use in individuals with Type 2 diabetes. Additionally, Tirzepatide has been associated with weight loss, with a dose-dependent relationship, and some individuals experiencing a weight loss of up to 11 kg (25 lbs) over six months.

Tirzepatide not only increases insulin levels but also appears to enhance the function of pancreatic beta cells, the cells responsible for producing and releasing insulin. This improvement in beta cell function can reduce stress on these cells and potentially slow the progression of Type 2 diabetes.

Interestingly, Tirzepatide acts in response to increased blood glucose levels. When blood glucose is elevated, Tirzepatide increases insulin levels, but it reduces insulin levels during fasting, thereby improving insulin sensitivity over time. It also decreases fasting levels of glucagon, which can exacerbate hyperglycemia by interfering with liver glucose metabolism. These combined effects contribute to Tirzepatide’s significant impact on glucose control and HbA1c levels.

Tirzepatide is a dual agonist of the gastric inhibitory polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R). GIPR and GLP-1R stimulation have synergistic effects that make Tirzepatide more effective than strict GLP-1 agonists in treating Type 2 diabetes. Tirzepatide has a higher affinity for the GIP receptor compared to the GLP-1 receptor. GIPR stimulation primarily leads to insulin release after meals, while GLP-1R stimulation not only promotes insulin synthesis and release but also increases beta cell density in the pancreas, promoting beta cell survival and insulin production.

Tirzepatide also appears to raise adiponectin levels, a peptide hormone associated with fat metabolism. Increased adiponectin levels reduce fat cell differentiation and enhance energy expenditure by making mitochondria less efficient. This can improve insulin sensitivity and help mitigate conditions such as Type 2 diabetes, atherosclerosis, and non-alcoholic fatty liver disease.

In terms of hunger regulation, Tirzepatide initially delays gastric emptying, leading to increased feelings of satiety and reduced hunger and food cravings. However, this effect diminishes over time due to tachyphylaxis. To address this, a low-dose start with a gradual escalation has been shown to prolong the gastric emptying delay, helping to alter eating patterns over time.

Tirzepatide is also associated with substantial weight loss over six months, which is in contrast to some other GLP-1 analogues that may cause weight gain. The GIP agonism of Tirzepatide appears to play a significant role in its long-term effects on weight. GIP activates receptors in fat cells, increasing insulin sensitivity, reducing adipose inflammation, and increasing adiponectin levels. Additionally, GIP signaling in the central nervous system regulates feeding centers in the hypothalamus, leading to decreased food intake and improved glucose handling, ultimately contributing to weight loss.

Overall, Tirzepatide’s multifaceted actions on insulin release, beta cell function, insulin sensitivity, hunger regulation, and weight loss make it a promising candidate for the treatment of Type 2 diabetes.

Tirzepatide, a synthetic derivative of gastric inhibitory polypeptide (GIP) with simultaneous glucagon-like peptide-1 (GLP-1) functionality, offers a range of potential benefits beyond its primary use in the treatment of Type 2 diabetes. These benefits extend to cardiovascular health and weight management:

  1. Heart Health: Tirzepatide can positively impact heart health by altering adiponectin levels. Increased adiponectin levels are associated with a decreased risk of atherosclerosis, obesity, and heart disease. Tirzepatide has been shown to improve lipoprotein biomarkers, reducing triglyceride levels, apoC-III, and other lipoproteins. This translates to a lower risk of heart disease, possibly through decreased adiposity. Higher adiponectin levels are linked to increased HDL (good cholesterol) and decreased triglycerides, both of which are heart-protective. Additionally, increased adiponectin levels can reduce scavenger receptors in macrophages and promote cholesterol efflux, providing further protection against atherosclerosis.

  2. GLP-1 and Cardiovascular Risk Factors: GLP-1, one of the components of Tirzepatide, plays a vital role in regulating cardiovascular risk factors such as hypertension, dyslipidemia, and obesity. It helps lower blood pressure, improve lipid profiles, and contribute to weight loss. The effect on endothelial function is noteworthy, with GLP-1 signaling leading to blood vessel relaxation, reduced blood pressure, and improved end-organ perfusion. GLP-1 signaling can also reduce inflammation, a key factor in atherosclerosis development.

  3. Inflammation Reduction: Inflammation is a significant contributor to atherosclerosis and cardiovascular disease. GLP-1 signaling has been shown to reduce inflammation through various mechanisms, including decreased NF-κB signaling, reduced MMP-9 activity, inhibition of inflammatory cytokine synthesis, and decreased inflammatory macrophage activity. These anti-inflammatory effects can last for several months after a single dose of a GLP-1R agonist like Tirzepatide.

  4. Clinical Trials for Heart Failure: Tirzepatide is currently undergoing clinical trials to further assess its medium-term effects on individuals with heart failure, indicating its potential as a treatment option for heart-related conditions.

In summary, Tirzepatide, initially developed for the treatment of Type 2 diabetes, demonstrates significant cardiovascular benefits by positively influencing risk factors such as adiponectin levels, blood pressure, lipid profiles, and inflammation. These effects can help reduce the risk of heart disease and improve overall cardiovascular health.

Article Author

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.


The product information featured on this website pertains exclusively to in-vitro studies. In-vitro studies, also known as ‘in glass’ studies, are conducted outside of living organisms. It’s important to emphasize that these products do not constitute medicines or drugs and have not received FDA approval for the prevention, treatment, or cure of any medical conditions, ailments, or diseases. It is crucial to note that the introduction of these products into the bodies of humans or animals is strictly prohibited by law.