Retatrutide - Triple GLP-1R / GIPR / GCGR Ligand - Sterile

Synthetic peptide analog - CAS #2381089-83-2

ABOUT

GLP-1R / GIPR / GCGR poly-agonist – CAS #2381089-83-2

Retatrutide (LY3437943) is a triple agonist of the GIP, GLP-1, and glucagon receptors that has reshaped 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, while glucagon signaling promotes energy expenditure. Retatrutide is currently under clinical investigation for the treatment of obesity, type 2 diabetes, and other metabolic disorders.

More details More details

Retatrutide is a synthetic 39-amino-acid peptide engineered from the native GIP sequence and modified to enable simultaneous activation of the GIP receptor (GIPR), GLP-1 receptor (GLP-1R), and glucagon receptor (GCGR). Structural modifications confer increased resistance to enzymatic degradation and extend its half-life to 150–180 hours, supporting once-weekly administration.

InvivoGen Retatrutide 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, HEK-Blue™ GIP, and HEK-Blue™ Glucagon expressing the GLP-1R, GIPR, or GCGR, 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 Retatrutide to GLP-1R, GIPR, and GCGR
Binding of Retatrutide to GLP-1R, GIPR, and GCGR

SPECIFICATIONS

Specifications

Source
Synthetic
Synonyms
LY3437943
CAS number
2381089-83-2
Molecular weight
4731.33 g/mol (free base)
Purity
≥ 95% (UHPLC)
Solubility

1 mM (4.73 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: C221H342N46O68 . Na
Short sequence: Y-{Aib}-QGTFTSDYSI-{α-Me-Leu}-LDK-{Lys(AEEA-γGlu-C20 diacid)}AQ-{Aib}-AFIEYLLEGGPSSGAPPPS 
Salt form: Sodium salt

CONTENTS

Contents

  • Product: 
    Retatrutide
  • Cat code: 
    hlc-reta
  • Quantity: 
    5 mg
Includes:

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

Shipping & Storage

    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/GCGR signaling and metabolic regulation

Peptide hormones acting through the glucagon-like peptide-1 receptor (GLP-1R), the glucose-dependent insulinotropic polypeptide receptor (GIPR), and the glucagon receptor (GCGR) play complementary roles in the regulation of glucose metabolism and energy balance [1]. In pancreatic β cells, activation of these G protein–coupled receptors primarily signals 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, coordinated GLP-1R, GIPR, and GCGR signaling also influence lipid metabolism and energy expenditure 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 Retatrutide

Exploitation of GLP-1R, GIPR, and GCGR signaling has driven the development of multi-receptor–targeted therapeutic strategies. Retatrutide (LY3437943) represents a major advance in this direction as a synthetic peptide designed to simultaneously activate GLP-1R, GIPR, and GCGR [2,3]. Retatrutide exhibits a prolonged circulating half-life of approximately 150–180 hours, enabling sustained multi-receptor engagement. Through coordinated activation of incretin and glucagon pathways, retatrutide enhances glucose-dependent insulin secretion, improves glycemic control, promotes lipid utilization and energy expenditure, and reduces appetite and food intake, highlighting its relevance for obesity and type 2 diabetes [2,3].

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. Kaur K & Misra S, 2024. A review of an investigational drug retatrutide, a novel triple agonist agent for the treatment of obesity. Eur J of Clin Pharm. 8:669-676. 
3. Rosenstock J et al., 2023. Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA.  Lancet. 402:529-44.

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