Orforglipron

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Cat Number

API2212020523

CAS Number

2212020-52-3

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Product Detail Description Scientific Support Customer Q&A

CAS Number

2212020-52-3

Storage

Store at -20℃

Synonyms

LY3502970; OWL833

Molecular Formula

C48H48F2N10O5

Molecular Weight

882.97

Smiles

C[C@H]1C[C@]1(C2=NOC(=O)N2)N3C4=C(C=C(C=C4)[C@H]5CCOC(C5)(C)C)C=C3C(=O)N6CCC7=NN(C(=C7[C@@H]6C)N8C=CN(C8=O)C9=C(C1=C(C=C9)N(N=C1)C)F)C1=CC(=C(C(=C1)C)F)C

Appearance

Solid

General Description

Orforglipron, an oral, non-peptide, first-in-class partial agonist of the GLP-1 receptor that selectively favors G protein activation over β-arrestin recruitment. Orforglipron elicits its GLP-1 mediated effects by decreasing appetite, slowing gastric emptying, and enhancing glycemic control.

Mechanism of Action

Orforglipron functions as an agonist of glucagon-like peptide-1 (GLP-1), a hormone that regulates glucose metabolism in the body. When administered, orforglipron activates GLP-1 receptors located on the pancreatic cells, which in turn stimulate insulin secretion in response to high blood sugar levels. Additionally, orforglipron inhibits the release of glucagon, another hormone that increases glucose production in the liver. Furthermore, it slows down the emptying of the stomach contents into the small intestine, thereby increasing satiety and reducing appetite.

Application

Orforglipron is an investigational, oral, non-peptide small-molecule GLP-1 receptor agonist currently in late-stage clinical development. It is primarily being evaluated for chronic weight management in adults with obesity and glycemic control in patients with type 2 diabetes. Furthermore, its potential therapeutic applications are expanding to address obesity-related complications, including obstructive sleep apnea, cardiovascular metabolic improvements, and stress urinary incontinence.

Orforglipron is a small-molecule compound that is a partial agonist of GLP-1R. Orforglipron robustly increased cAMP generation by Gs protein-mediated signaling but did not cause β-arrestin recruitment. This bias toward cAMP signaling over β-arrestin recruitment is associated with persistent receptor sensitivity and could blunt some of the (AEs) often seen with full GLP-1R agonists.

Fig. 1 Structural classes, receptor engagement, and signaling outcomes of GLP-1R agonists. (Saldívar-Cerón H I, et al. 2025)

References

Saldívar-Cerón H I, et al. Oral small-molecule GLP-1 receptor agonists: Mechanistic insights and emerging therapeutic strategies. Scientia Pharmaceutica. 2025, 93(2): 26.

Does Orforglipron require protection from direct light during storage?

Yes, Orforglipron powder must be kept in light-resistant containers.

How can I track my Orforglipron shipment after dispatch?

We provide a tracking number for your Orforglipron immediately.

What documentation is provided with an Orforglipron batch?

Each Orforglipron batch comes with a COA.