Publish Time: 2021-09-30 Origin: Site
liraglutide is a glucagon-like peptide-1 (GLP-I) receptor agonist, similar to GLP-I in terms of molecular structure, biological activity, the target of the action, and immunogenicity. The molecular structure of liraglutide is similar to that of GLP-I (7-36). The difference is that liraglutide replaces the 34th lysine of GLP-I with arginine and adds the second place One palmitoyl fatty acid side chain.
What are the advantages of liraglutide?
What are the pharmacological effects of liraglutide?
What is the value of liraglutide?
What are the advantages of liraglutide?
Polypeptide drugs generally have short half-lives in the body, poor physical and chemical stability, and are easily degraded by various proteases in the body. As a subcutaneous injection preparation, liraglutide has a half-life of about 12 to 14 hours. It needs to be used once a day. It has a good effect on lowering blood sugar, but it brings a greater burden to the patient's body, psychology, and economy, and limits the patient's compliance with medication. Therefore, structural modification of liraglutide and the development of new dosage forms to extend its plasma cycle and increase its systemic drug exposure are of great significance.
What are the pharmacological effects of liraglutide?
liraglutide is a GLP-1 analog with 97% sequence homology to human GLP-1. Human GLP-1 can bind to and activate the GLP-1 receptor. The GLP-1 receptor is the target of natural GLP-1. GLP-1 is an endogenous incretin hormone that can promote glucose concentration-dependent secretion of insulin from pancreatic β cells. Different from natural GLP-1, the pharmacokinetic and pharmacodynamic characteristics of liraglutide in humans are suitable for the once-a-day dosing regimen. After subcutaneous injection, the mechanism of prolonged action time includes self-association that slows absorption; binding to albumin; Higher enzyme stability, which has a longer plasma half-life.
What is the value of liraglutide?
Relevant data of patients.
liraglutide is the first and currently the only human GLP-1 analogue, which has a long-lasting effect. When nutrients are taken orally, glucagon-like peptide-1 can promote the secretion of insulin, but the human body's GLP-1 can be used by dipeptidyl enzyme -4 (DPP-4) degrades rapidly. liraglutide is a complete agonist of the GL_P-1 receptor, and its 97% amino acid sequence is identical to that of the human GLP-1 molecule. In terms of human structure, there are only two differences between the two molecules. First, the C16 fatty acid is linked to lysine via glutamic acid at position 26. Secondly, the lysine is replaced by arginine in the 34th position to ensure that the C16 side chain can only bind to the 26th position. The fatty acid side chain can make liraglutide reversibly bind to albumin in the blood, prolong the action time of liraglutide, and enhance the resistance to DPP-4 enzymatic degradation. The fatty acid side chain
It is not allowed to self-crosslink the liraglutide molecule into a heptamer at the injection site, thereby delaying its subcutaneous attraction, so that its action time can be as long as 24 hours. It is injected once a day and can be injected at any time, regardless of the meal. It is suitable for adults with type 2 diabetes. It regulates blood sugar in a glucose concentration-dependent manner, directly protects B cells, increases insulin secretion and reduces improper glucagon secretion by a-cells, and reduces body weight by improving satiety and reducing caloric intake. The sooner the systolic blood pressure is reduced, the better. liraglutide is a revolutionary drug in the treatment of type 2 diabetes.
The increase in diabetes does not allow the increase in liraglutide. Chengdu Pukang Company is a company specializing in the production of liraglutide. Here, you can order high-quality liraglutide.