Orforglipron - Oral GLP-1R Ligand - Sterile

Synthetic small molecule - CAS #2212020-52-3

ABOUT

Selective, orally available GLP-1R agonist - CAS #2212020-52-3

Orforglipron (LY3502970) is an orally active small molecule that has reshaped obesity and diabetes research. This investigational drug selectively activates the glucagon-like peptide-1 receptor (GLP-1R), a key regulator of energy balance. GLP-1R activation enhances glucose-dependent insulin secretion, suppresses glucagon release, delays gastric emptying, and promotes satiety. As such, GLP-1 signaling has become a major therapeutic strategy for metabolic disorders.

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InvivoGen Orforglipron is highly pure and guaranteed sterile making it suitable for in vivo studies. The biological activity is validated using a colorimetric bioassay consisting of an engineered cell line HEK-Blue™ GLP-1, expressing the GLP-1R together with a CREB-inducible SEAP reporter gene (see figure).

 

Key features

  • Each lot is validated using HEK-Blue™ GLP-1 cells
  • 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 Orforglipron to GLP-1R
Binding of Orforglipron to GLP-1R

SPECIFICATIONS

Specifications

Source
Synthetic
Synonyms
LY3502970
CAS number
2212020-52-3
Molecular weight
882.96 g/mol
Purity
≥ 95 % (UHPLC)
Solubility

10 mM (8.82 mg/mL) in DMSO 

Appearance (form)
Dried
Reconstitution buffer
DMSO (not 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: C48H48F2N10O5 

CONTENTS

Contents

  • Product: 
    Orforglipron
  • Cat code: 
    hlc-orfo
  • Quantity: 
    5 mg

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 signaling and metabolic regulation

Peptide hormones acting through the glucagon-like peptide-1 receptor (GLP-1R) play a central role in the regulation of glucose metabolism and energy balance [1]. In pancreatic β cells, GLP-1R activation signals primarily through G protein–coupled receptor 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 its insulinotropic effects, GLP-1R signaling also influences lipid metabolism by modulating hepatic lipid handling and adipose tissue function. Dysregulation of GLP-1R signaling contributes to impaired insulin secretion, altered lipid homeostasis, hyperglycemia, and metabolic dysfunction observed in obesity and type 2 diabetes [1].

Therapeutic relevance of Orforglipron

Exploitation of GLP-1R signaling has driven the development of GLP-1R–targeted therapies. Orforglipron (LY3502970) represents a significant advance in this direction as a synthetic small-molecule GLP-1R agonist optimized for oral delivery and metabolic stability [2]. While peptide-based GLP-1R agonists such as Semaglutide have transformed the treatment landscape, their injectable administration has stimulated interest in orally available alternatives. 

Orforglipron's design confers high resistance to enzymatic degradation and extends its circulating half-life to approximately 29–49 hours, enabling sustained receptor engagement in clinical trials. Through GLP-1R activation, Orforglipron 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 [2].

1. Zheng Z. et al., 2024. Glucagon-like peptide-1 receptor: mechanisms and advances in therapy. Sig Transduct Target Ther. 9, 234.
2. Horn D.B. et al., 2025. Orforglipron, an oral small-molecule GLP-1 receptor agonist, for the treatment of obesity in people with type 2 diabetes (ATTAIN-2): a phase 3, double-blind, randomised, multicentre, placebo-controlled trial. The Lancet. 406(10522): 2927-2944.

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