GLP-1 (Orforglipron) 5 mg

Orforglipron GLP-1 reagent - characteristics

Orforglipron (LY-3502970) is a synthetic, low-molecular-weight, non-peptide GLP-1 receptor agonist belonging to the G-protein-coupled receptor (GPCR) ligands. It is designed as a stable organic compound that allows effective oral administration. The molecule selectively interacts with the transmembrane domain of the GLP-1 receptor, leading to its activation through an allosteric-agonistic mechanism and activation of G-protein and β-arrestin-dependent signalling pathways. The non-peptide nature provides resistance to enzymatic degradation, including lack of susceptibility to DPP-4, and promotes favourable bioavailability. The compound provides a useful research tool in the analysis of structure-activity relationship (SAR) and mechanisms of GPCR receptor activation by small-molecule ligands. Functionally, the compound is being designed as an oral alternative to injectable incretin axis agonists that exhibit complex metabolic activity, such as semaglutide, tirzepatyd or retatrutide.

Mechanism of action of Orforglipron

Orforglipron acts as GLP-1 receptor agonist - This compound binds to the GLP-1 receptor on pancreatic β-cells and in other tissues involved in energy regulation, activating a signalling cascade leading to, among other things, increased cAMP levels and enhanced glucose-dependent insulin secretion. In vitro and in vivo studies have shown that orforglipron, as a non-peptide agonist, has a different signalling profile compared to classical GLP-1 peptide analogues - including different activity towards β-arrestin. These differences may translate into the specificity and extent of observed pharmacological effects under experimental conditions.

In the phase 2 and 3 clinical trials described in the scientific article NEJMoa2511774, a significant effect resulting from the use of orforglipron was observed, In addition, in the conducted research improvements in metabolic parameters such as waist circumference, blood pressure and lipid profile were observed. The most common side effects were of a gastrointestinal nature and were in line with the profile known for GLP-1 drugs. Preliminary results from clinical trials indicate that Orforglipron could become a breakthrough in the segment of oral substances supporting research on people battling obesity and type 2 diabetes.

Orforglipron is an oral, small-molecule GLP-1 receptor agonist that was administered once daily in tablet form in clinical trials. Publications describe oral administration regimens without significant meal-time restrictions.

Predicted/estimated price of Orforglipron

•  The retail price of orforglipron is not yet precisely known.
• According to a Polish media forecasting source, the price of orforglipron could be around PLN 900-1200 per month if it is launched on the Polish market.
• At the same time, it is important to stress that these are estimates - the final price will depend on many factors: production costs, pricing strategy, reimbursement in the country.
• Orforglipron is currently only available in the context of clinical and laboratory trials, and the estimated price of the formulation is more than US$300 per month for 60 10mg capsules.

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The product is intended for scientific research and laboratory analysis. All articles and information on this website are for informational and educational purposes only.