Introduction and application of  CAS No. 204656-20-2 | Liraglutide

Synonyms:Glycine,L-histidyl-L-alanyl-L-alpha-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha-aspartyl-L-valyl-L-seryl-L-seryl-L-tyrosyl-L-leucyl-L-alpha-glutamylglycyl-L-glutaminyl-L-alanyl-L-alanyl-N6-(N-(1-oxohexadecyl)-L-gamma-glutamyl)-L-lysyl-L-alpha-glutamyl-L-phenylalanyl-L-isoleucyl-L-alanyl-L-tryptophyl-L-leucyl-L-valyl-L-arginylglycyl-L-arginyl-;

Liraglutida;

Liraglutida[inn-spanish];

Liraglutide[usan:inn];

Liraglutidum;

Liraglutidum[inn-latin];

N26-(Hexadecanoyl-gamma-glutamyle)-(34-arginine)glp-1-(7-37)-peptide

Specification:

Overview:

Liraglutide is a clear, colorless solution. The dosage form is subcutaneous injection. After more than 10 years of research and development, Liraglutide has many functions such as promoting islet cell regeneration, lowering blood sugar, reducing weight and protecting the cardiovascular system. The trade name Victoza is used to treat type 2 diabetes, and the trade name Saxenda is used to treat chronic obesity. As a supplement to diet and physical exercise. Liraglutide is an acylated human glucagon-like peptide-1 (GLP-1) receptor agonist that has 97% amino acid sequence homology with human endogenous GLP-1 (7-37) and retains It has all the biological activities of GLP-1 and has GLP-1 receptor agonism. Through the expression of recombinant DNA in Saccharomyces cerevisiae, its molecular structure has only one amino acid difference from the natural GLP-1 molecule. The structure only has the following two modifications to GLP-1: Lysine at position 34 is replaced by arginine. Acid substitution, in addition, a glutamate-mediated 16-carbon palmitoyl fatty acid side chain is added to lysine 26.

Mechanism:

Liraglutide, like endogenous GLP-1, binds to and activates the GLP-1 receptor, a cell surface receptor that activates adenylyl cyclase via excitatory G protein Gs coupling. Endogenous GLP-1 has a half-life of 1.5~2 minutes and is easily degraded by two widely existing endogenous enzymes, dipeptidyl peptidase 4 (DPP-4) and neutral endopeptidase (NEP). Compared with natural GLP-1, liraglutide is relatively stable, with a plasma half-life of 13 hours after subcutaneous administration. This change in half-life is attributed to the modification of the structure of liraglutide. Due to the presence of fatty acid side chains, on the one hand, the hydrophobicity of palmitic acid self-associates into a heptamer, which slows down the absorption at the subcutaneous injection site; on the other hand, absorption After entering the blood, it increases its binding to plasma albumin, forming a slow-release reservoir. It temporarily avoids contact with endogenous enzymes and slows down the release, prolonging the absorption and distribution time in the body, and its half-life is significantly longer than that of natural GLP-1

Pharmacological effects Liraglutide has the following pharmacological effects:

Protective effect on pancreatic beta cells

Effect of reducing body weight

Liraglutide’s cardiovascular effects

Protective effect on liver

Therapeutic effect on Alzheimer's disease (AD)

Package and transportation :

Package: 10g,25g,50g,100g,250g

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