リラグルチド

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

リラグルチド 化学特性,用途語,生産方法

• 用途

  リラグルチド（Liraglutide）は2型糖尿病治療用の長期作用型ヒトGLP-1アナログ製剤の1つである。血糖値の高い場合にのみインスリン分泌効果等を発揮し、臨床的に有意な血糖降下作用を示す。ただし、インスリンの代替薬としては使用できない。

• 化学的特性

  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.

• 使用

  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.

• 定義

  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.

• 一般的な説明

  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).

• 生物活性

  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.

• 副作用

  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.

• 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.

リラグルチド 生産企業

Global(441)Suppliers

リラグルチド スペクトルデータ(MS)

204656-20-2, リラグルチド キーワード