Orforglipron Base

Orforglipron is a nonpeptide agonist of the glucagon-like peptide 1 receptor (GLP-1R) developed for once-daily oral administration in type 2 diabetes and obesity. As the first oral small molecule GLP-1 receptor agonist to successfully complete a Phase 3 trial, Orforglipron represents a paradigm shift in GLP-1-based therapeutics. Orforglipron can be used for analytical method development, method validation (AMV), and quality control (QC) applications. Additionally, Orforglipron is under investigation in clinical trials.

Product Parameters

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Parameter	Specification
Product Name	Orforglipron Base
CAS Number	2212020-52-3
Molecular Formula	C₄₈H₄₈F₂N₁₀O₅
Molecular Weight	882.97 g/mol
Density	1.50 ± 0.1 g/cm³ (predicted)
Storage Condition	Store at –20 °C

 

Oral non-peptide drugs

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Orforglipron belongs to a novel class of chemically synthesized oral non-peptide drugs that exert potent antidiabetic effects by enhancing glucose-dependent insulin secretion and improving energy balance. In preclinical models, orforglipron demonstrated significant efficacy in reducing hyperglycemia in experimental animals and exhibits favorable pharmacokinetic characteristics for oral administration.

 

Oraglinide, currently used to improve glycemic control in adults and manage chronic weight issues (weight loss), initiated Phase 3 clinical trials in September 2023. Results from Phase 1 studies demonstrated its GLP-1-like effects, indicating efficacy in treating obesity and type 2 diabetes comparable to other GLP-1 analogs. Phase 2 data showed that oraglinide significantly reduced HbA1c levels and body weight, with no clinically significant adverse events observed that differed from those associated with other GLP-1 receptor agonists. Its pharmacokinetic profile permits once-daily oral administration without dietary restrictions regarding food or water intake, offering a safe and effective oral treatment option for patients with type 2 diabetes and other conditions [1]. Currently, the standard administration route is subcutaneous injection; however, oral formulations provide greater convenience and accessibility compared to injectable formulations and may alleviate concerns about injections among some patients.

 

Bioactivity

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Orforglipron (LY3502970) (Compound 67) is an orally effective glucagon-like peptide 1 receptor (GLP-1R) agonist that improves type 2 diabetes.

 

FAQ

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Q1: What is the primary target of Orforglipron?

A: Orforglipron is a nonpeptide agonist of the glucagon-like peptide 1 receptor (GLP-1R). It is a chemically synthesized, small-molecule partial agonist.

 

Q2: What is the EC₅₀ of Orforglipron for GLP-1R?

A: Orforglipron induces cAMP accumulation in HEK293 cells expressing human GLP-1R with an EC₅₀ of 3.05 nM.

 

Contact Us

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Acquiring Orforglipron for your metabolic disease research, GLP-1R pharmacology studies, or analytical method development should be a seamless experience. Cosperpharm is here to support your work. Get in touch with us today to discuss your specific needs.