Liraglutide

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Liraglutide Chemische Eigenschaften,Einsatz,Produktion Methoden

• Chemische Eigenschaften

  Liraglutide is characterized as a white to almost white powder. It is freely soluble in aqueous base solutions (> 270 mg/mL), but its water solubility decreases below pH 7 and reaches its lowest level at pH 4-5 (approximately 0.05 mg/mL). Solubility increases marginally at pH 2.5 where it is very slightly soluble (≤ 0.8 mg/mL). Liraglutide is soluble in methanol (68 mg/mL) and very slightly soluble in ethanol (1.1 mg/mL). The isoelectric point of liraglutide is approximately 4.9. The pH of a 1 mg/mL aqueous solution of drug substance is approximately 9.3.

• Originator

  Massachusetts General Hospital (US)

• Verwenden

  Liraglutide is a new type of hypoglycemic drug that activates AMP-activated protein kinase thus enhancing insulin sensitivity. It not only has a significant hypoglycemic effect, but also has the functions of weight loss, blood pressure reduction, and improvement of blood lipid profile.
  Liraglutide, a human glucagon-like peptide-1 (GLP-1) receptor agonist, slows gastric emptying, increases satiety, and reduces patient eating, while reducing the brain's desire to eat and allowing the body to Increased energy expenditure plays a role in weight loss; it prevents the liver from producing too much glucose and promotes the pancreas to produce more insulin to lower blood sugar; in addition, liraglutide also has cardiovascular benefits and kidney protection.

• Definition

  ChEBI: Liraglutide, a lipopeptide and polypeptide, is an analogue of human GLP-1 in which the lysine residue at position 27 is replaced by arginine and a hexadecanoyl group attached to the remaining lysine via a glutamic acid spacer. It is used alongside diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Liraglutide functions as a glucagon-like peptide-1 receptor agonist and serves as a neuroprotective agent.

• Trademarks

  Victoza

• Allgemeine Beschreibung

  Liraglutide is GLP-1(1–37) modified at Ly: the -amino group is acylated with an (N-hexadecanoyl)glutam- -yl moiety that noncovalently but avidly binds tohuman serum albumin. (Also, Lys is conservatively replacedwith Arg.) These changes provide for a greatly extendedserum t1?2 of～10 to 15 hours after sc administration(0.6–1.8 mg), allowing for once-daily dosing.Liraglutide (Victoza, Novo Nordisk) is awaiting approvalby the FDA, EMEA, and the Koˉ roˉ -shoˉ (Japan).

• Biologische Aktivität

  Liraglutide is a highly potent, long-acting GLP-1 receptor agonist (EC50 = 61 pM). Acylated derivative of GLP-1 (7-37) (Cat. No. 5374). Inhibits food and water intake, causing lasting and reversible weight loss in normal and obese rats. In an animal model of Alzheimer's disease, Liraglutide decreases levels of Aβ and soluble amyloid, and reduces neuroinflammation.

• Clinical Use

  Glucogen-like peptide-1 analogue:
  Treatment of type 2 diabetes mellitus in combination with other antidiabetic therapy

• Nebenwirkungen

  The most frequent adverse events associated with liraglutide therapy were gastrointestinal in nature, in accordance with GLP-1 receptor activation, and included nausea, diarrhea, vomiting, constipation, abdominal pain, and dyspepsia.

• Lager

  Store at -20°C

• Clinical claims and research

  Liraglutide, the GLP-1 receptor agonist to reach the market, possesses a 97% homology to GLP-1 with only two amino acid changes and the addition of a fatty acid side chain. Specifically, the lysine in position 34 has been replaced with an arginine, and the lysine in position 26 has been modified with a C16 acyl chain via a glutamoyl spacer. Liraglutide derives its resistance to DPP-4 degradation from its propensity to form micelles and to bind to albumin. Unlike its predecessor exenatide, which requires two daily subcutaneous injections before the first and last meals of the day, liraglutide is approved as a once-daily treatment regimen and may be used in combination with metformin or a sulfonylurea in patients with insufficient glycemic control with either monotherapy or combined dual therapy. It is also approved in combination with the dual therapy of metformin and a thiazolidinedione in patients with insufficient glycemic control. Liraglutide displayed a binding potency of 61 pM (EC50= 55 pM for GLP-1) for the cloned human GLP-1 receptor.

• Mode of action

  Liraglutide is an acylated human glucagon-like peptide-1 (GLP-1) receptor agonist with 97% amino acid sequence homology to endogenous human GLP-1(7-37). Like endogenous GLP-1, liraglutide binds to and activates the GLP-1 receptor, a cellsurface receptor coupled to adenylyl cyclase activation through the stimulatory G-protein, Gs. Endogenous GLP-1 has a half-life of 1.5-2 minutes due to degradation by the ubiquitous endogenous enzymes, dipeptidyl peptidase 4 (DPP-4) and neutral endopeptidases (NEP). Unlike native GLP-1, liraglutide is stable against metabolic degradation by both peptidases and has a plasma half-life of 13 hours after subcutaneous administration.

Liraglutide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(445)Suppliers

204656-20-2, Liraglutide Verwandte Suche: