Tirzepatide - Dual GLP-1R / GIPR Ligand - Sterile

Synthetic peptide analog - CAS # 2023788-19-2

ABOUT

GLP-1R/GIPR agonist – CAS #2023788-19-2

Tirzepatide (LY3298176) is a long-acting dual agonist of the GIP and GLP-1 receptors that has transformed obesity and diabetes research. GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide) are incretin hormones that regulate glucose homeostasis by stimulating glucose-dependent insulin secretion, slowing gastric emptying, and reducing appetite. Tirzepatide has been approved by the FDA for the treatment of type 2 diabetes (Mounjaro®) and chronic weight management (Zepbound®).

More details More details

Tirzepatide is a synthetic 39-amino-acid peptide engineered from the native GIP sequence and modified to enable dual activation of the GIP receptor (GIPR) and the GLP-1 receptor (GLP-1R). Structural modifications confer increased resistance to enzymatic degradation and extend its half-life to 120–150 hours, supporting once-weekly administration.

InvivoGen Tirzepatide is highly pure and guaranteed sterile, making it suitable for in vivo studies. The biological activity can be assessed using colorimetric bioassays consisting of engineered cell lines HEK-Blue™ GLP-1 and HEK-Blue™ GIP expressing the GLP-1R or GIPR, respectively, together with a CREB-inducible SEAP reporter gene (see figure). 

Key features

  • Each lot is validated using proprietary incretin bioassay
  • Guaranteed sterile 
  • No ultrasonication step needed
  • Endotoxin-tested 

 

Illustrations on this page were created with BioRender.com.

All products are for research use only, and not for human or veterinary use.

Binding of Tirzepatide to GLP-1R and GIPR
Binding of Tirzepatide to GLP-1R and GIPR

SPECIFICATIONS

Specifications

Source
Synthetic
Synonyms
LY3298176
CAS number
2023788-19-2
Molecular weight
4813.30 g/mol
Purity
≥ 95% (UHPLC)
Solubility

1 mM (4.81 mg/ml) in water or physiological water 

Appearance (form)
Lyophilized
Reconstitution buffer
Endotoxin-free physiological water (provided)
Sterility

0.22 µm filtration, Sterility guaranteed

Endotoxin

The absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ TLR2 and HEK‑Blue™ TLR4 cells.

Applications

Cellular assays (tested)

In vivo assays

Quality control

Each lot is functionally tested and validated.

Additional information

Chemical formula: C225H348N48O68 
Short sequence: Y-{Aib}-EGTFTSDYSI-{Aib}-LDKIAQ-{C20 diacid-gamma-Glu-(AEEA)2-Lys}-AFVQWLIAGGPSSGAPPPS 
 

CONTENTS

Contents

  • Product: 
    Tirzepatide
  • Cat code: 
    hlc-tirz
  • Quantity: 
    5 mg
Includes:

1.5 ml sterile endotoxin-free physiological water (NaCl 0.9%)

Shipping & Storage

  • Shipping method:  Room temperature

    • Storage:

    • -20°C
    • -80°C
    Stability: Resuspended product is stable for 6 months at -20°C.

    Caution:

    • Avoid repeated freeze-thaw cycles

Details

GLP-1R/GIPR signaling and metabolic regulation

Peptide hormones acting through the glucagon-like peptide-1 receptor (GLP-1R) and the glucose-dependent insulinotropic polypeptide receptor (GIPR) play complementary roles in the regulation of glucose metabolism and energy balance [1]. In pancreatic β cells, activation of these G protein–coupled receptors is primarily mediated through pathways involving cyclic adenosine monophosphate (cAMP), protein kinase A (PKA), and cAMP response element–binding protein (CREB), thereby enhancing glucose-dependent insulin secretion and supporting β-cell function. 

Beyond their insulinotropic effects, GLP-1R and GIPR signaling also influences lipid metabolism by modulating hepatic lipid handling and adipose tissue function. Dysregulation of these pathways contributes to impaired insulin secretion, altered lipid homeostasis, hyperglycemia, and metabolic dysfunction observed in obesity and type 2 diabetes [1].

Therapeutic relevance of Tirzepatide

Exploitation of GLP-1R and GIPR signaling has driven the development of dual-receptor–targeted therapies. Tirzepatide represents a major advance in this direction as a synthetic peptide designed to simultaneously activate GLP-1R and GIPR [2]. It has received U.S. Food and Drug Administration (FDA) approval for the treatment of type 2 diabetes (Mounjaro®) and for chronic weight management (Zepbound®). 

While peptide-based GLP-1R agonists such as semaglutide have transformed the treatment landscape, dual incretin receptor engagement further enhances metabolic outcomes. Tirzepatide exhibits a prolonged circulating half-life of approximately 120–150 hours, enabling sustained receptor engagement [3]. Through coordinated GLP-1R and GIPR activation, tirzepatide enhances glucose-dependent insulin secretion, improves glycemic control, contributes to lipid homeostasis, and reduces appetite and food intake, supporting its clinical use in obesity and type 2 diabetes [1–3].

1. Gutgesell RM et al., 2024. Dual and Triple Incretin-Based Co-agonists: Novel Therapeutics for Obesity and Diabetes. Diabetes Ther. 15(5):1069-1084.
2. Chavda V et al., 2022. Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review. Molecules. 27:4315.
3. Jastreboff AM et al., 2022. Tirzepatide once weekly for the treatment of obesity. N Engl J Med. 387:205–216.
 

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