The potential mechanism of G protein-coupled receptor 119 (GPR119) in regulating glucose homeostasis makes it an attractive target for antidiabetic drugs. Ace Therapeutics is committed to accelerating the development process of GPR119 agonists for our clients with a broad range of diabetes models and comprehensive preclinical testing capabilities. Our experienced team of experts provides comprehensive services from target validation to preclinical evaluation, enabling clients worldwide to efficiently develop novel GPR119 agonists.

GPR119 as Potential Antidiabetic Drug Targets

G protein-coupled receptor 119 (GPR119) is a promising new target for the treatment of type 2 diabetes mellitus (T2DM). Pharmacological activation of GPR119 produces pleiotropic beneficial effects, including：

• Stimulation of insulin secretion from pancreatic β-cells.
• Enhancement of glucagon-like peptide (GLP)-1 secretion from intestinal L cells.
• Glucose-dependent insulin secretion.
• Suppression of food intake and body weight gain.

Fig. 1 Mechanism of GPR119. (Dhankhar, S. et al., 2023)

Many pharmaceutical companies have been active in the search for GPR119 agonists, making it a highly competitive area in the industrial environment. A study has shown that a novel small molecule GPR119 agonist NCP-322 can effectively promote the secretion of insulin and GLP-1, and significantly reduce blood glucose fluctuations during hyperglycemia in an oral glucose tolerance test. These results suggest the promising therapeutic potential of NCP-322 for T2DM treatment.

Fig. 2 Pharmacological profile of NCP-322: a novel oral GPR119 agonist for type 2 diabetes mellitus. (Nakamura, H. et al., 2025)

GPR119 Agonist Development Services at Ace Therapeutics

Ace Therapeutics provides customized strategies tailored to the specific stage of our clients' drug development programs. Our objective is to support clients in identifying potential GPR119 agonists for antidiabetic drug development, while evaluating their efficacy, pharmacological properties, pharmacokinetics, and safety profiles, thereby enhancing the probability of successful development.

GPCR119 Target Validation and Mechanistic Research Services

Preclinical Screening Services of GPR119 Agonists

• Virtual screening

We use virtual screening technology to accurately dock molecules to GPR119 in compound libraries, simulate and evaluate their interaction mechanisms. With our advanced computational platform, we are able to efficiently screen candidate compounds that are highly compatible with the GPR119 binding pocket.

• High-throughput screening

Our cell-based high-throughput screening technology allows us to assay the activity and toxicity of thousands of compounds in a short period of time and rapidly identify promising GPR119 agonists.

Structural Optimization of GPCR 119 Agonists

• Structure-activity-relationship (SAR) studies

Ace Therapeutics guides the structural optimization of compounds by synthesizing and testing a series of structurally similar compounds to determine their active moieties and conformational relationships.

• Pharmacokinetic (PK) studies

We optimize the pharmacokinetic properties of GPR119 agonists candidate by assessing the absorption, distribution, metabolism and excretion (ADME) properties of the lead compound.

Preclinical Assessment of GPCR 119 Agonists

• Pharmacodynamic (PD) studies

We evaluate the hypoglycaemic effect of our GPR119 agonist candidate and its effect on insulin secretion by in vivo and in vitro tests.

• Toxicological evaluation

We evaluate the acute toxicity, subacute toxicity, and long-term toxicity of our GPR119 agonist candidate to ensure its safety.

• Safety pharmacology study

We comprehensively assess the safety of our GPR119 agonist candidate by studying its effects on the cardiovascular, respiratory, and central nervous systems.

Advantages of Our GPR119 Agonist Development Services

• Multidimensional validation from molecular level to tissue specificity.
• Flexible adjustment of the experimental program according to clients' needs.
• Enriched in vivo and in vitro diabetes models.

Ace Therapeutics is able to design and conduct efficient and cost-effective studies for our clients based on our extensive experience in diabetes modelling and antidiabetic drug development. Our expertise will accelerate the development of novel GPR119 agonists. Please contact us today. We are dedicated to providing our clients with the quality services that will help them succeed in their drug discovery and development endeavors.

References

1. Dhankhar, S.; et al. Novel targets for potential therapeutic use in Diabetes mellitus. Diabetology & Metabolic Syndrome. 2023, 15(1): 17.
2. Nakamura, H.; et al. Pharmacological Profile of NCP-322, a Novel G Protein-Coupled Receptor 119 Agonist, as an Orally Active Therapeutic Agent for Type 2 Diabetes Mellitus. Biological and Pharmaceutical Bulletin. 2025, 48(1): 65-74.
3. Ritter, K.; et al. G protein-coupled receptor 119 (GPR119) agonists for the treatment of diabetes: recent progress and prevailing challenges. Journal of medicinal chemistry. 2016, 59(8): 3579-3592.

• GIP-Targeted Drug Development for Diabetes
• THR-Targeted Drug Development for Diabetes
• GR-Targeted Drug Development for Diabetes
• PPARγ-Targeted Drug Development for Diabetes
• FFAR1-Targeted Drug Development for Diabetes
• GLP-1-Targeted Drug Development for Diabetes

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