GPR119 InhibitorChemicals ResearchUpdated on May 30, 2019 View more like this | Visit SHIRLEY, NY | Contact BOCSCI INC |
Inhibition of GPR119
GPR119 agonists can stimulate glucose-dependent insulin and glucagon-like peptide-1 release by increasing the level of intracellular cyclic adenosine monophosphate, lowering blood glucose levels and protecting islet β-cell viability, and effectively improving glucose balance in patients. According to clinical phase I trials, GPR119 agonists as a novel mechanism of action for antidiabetic drugs can significantly reduce the risk of hypoglycemia. In addition, GPR119 agonists are highly lipophilic, and this property is liable to cause cytotoxicity of the drug, causing biosafety problems. Therefore, GPR119 will become an ideal target for the development of anti-type 2 diabetes drugs. However, due to the toxicity caused by the high lipophilicity of the GPR119 agonist, its further development is limited. Therefore, in the design and development of the follow-up GPR119 agonist, attention should be paid to the structural modification while ensure the efficacy of the drug, pay attention to the ligand-lipophilic efficiency, reduce its lipophilicity, and ensure the safety of the drug.
GPR119 agonists can stimulate glucose-dependent insulin and glucagon-like peptide-1 release by increasing the level of intracellular cyclic adenosine monophosphate, lowering blood glucose levels and protecting islet β-cell viability, and effectively improving glucose balance in patients. According to clinical phase I trials, GPR119 agonists as a novel mechanism of action for antidiabetic drugs can significantly reduce the risk of hypoglycemia. In addition, GPR119 agonists are highly lipophilic, and this property is liable to cause cytotoxicity of the drug, causing biosafety problems. Therefore, GPR119 will become an ideal target for the development of anti-type 2 diabetes drugs. However, due to the toxicity caused by the high lipophilicity of the GPR119 agonist, its further development is limited. Therefore, in the design and development of the follow-up GPR119 agonist, attention should be paid to the structural modification while ensure the efficacy of the drug, pay attention to the ligand-lipophilic efficiency, reduce its lipophilicity, and ensure the safety of the drug.
