As the incidence of obesity and type 2 diabetes continues to rise worldwide, the development of new therapeutic drugs has attracted much attention. Orforglipron, as an oral small molecule glucagon-like peptide-1 (GLP-1) receptor agonist, has attracted a lot of attention since it entered the field of development. Its unique mechanism of action and potential therapeutic effect are expected to bring new changes to the treatment of metabolic diseases.

I. Mechanism of action

The central mechanism of action of oglitazone is based on the activation of the GLP-1 receptor. GLP-1 is a peptide hormone secreted by human intestinal cells. It is released after eating and can participate in a variety of physiological processes such as blood glucose regulation. By binding to the GLP-1 receptor and simulating the action of GLP-1, oglitazone exerts its efficacy in multiple dimensions.

1. It stimulates insulin release from pancreatic beta cells. Insulin is a key hormone to regulate blood glucose. It can promote the uptake and utilization of glucose in the blood by various tissues of the body, such as muscle, fat and liver, so as to effectively reduce blood glucose levels. Moreover, the "smart" property of ogaglione to stimulate insulin secretion only acts when blood glucose is elevated (such as after eating), and its stimulating effect is weakened when blood glucose is in the normal range, which greatly reduces the risk of hypoglycemia and makes blood glucose regulation more precise and safe.

2. Ogagliflozin can inhibit glucagon secretion by islet α-cells. Glucagon, which has the opposite effect of insulin, prompts the liver to release glucose into the blood, causing blood sugar to rise. By inhibiting glucagon secretion, ogagliflozin further reduces endogenous glucose production and controls the rise in blood glucose at its source.

3. In addition to regulating blood glucose, ologlitone is also effective in weight management. It can delay gastric emptying, allow food to stay in the stomach longer, slow down the speed of entering the small intestine, so that the digestion and absorption of carbohydrates slow down, avoid the sharp rise in postprandial blood sugar. At the same time, the delay of gastric emptying will send a satiety signal to the brain, reduce the desire to eat, reduce food intake, and achieve weight loss in the long term.

2. Basic information

English name: GLP-1 receptor agonist 1

Chinese name: Oglitazone

CAS No. : 2212020-52-3

Molecular formula: C48H48F2N10O5

Molecular weight: 882.97

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