Albiglutide Fragment

製品コードS3734 バッチS373401

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C148H224N40O45

分子量 3283.6 CAS No. 782500-75-8
Solubility (25°C)* 体外 Water 100 mg/mL (30.45 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Albiglutide fragment is one copy of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36).
in vitro

Albiglutide is a recombinant fusion protein consisting of two copies of a 30-amino-acid sequence of modified human GLP-1 (fragment 7-36), modified with a glycine substituted for the naturally occurring alanine at position 8 in order to augment resistance to DPP-4[1].

in vivo

Glucose lowering occurs within 24 h after a single dose of albiglutide, as a result of binding of the molecule to the GLP-1 receptor. The reduction in both fasting and postprandial glucose levels is dose related. Albiglutide is less potent than GLP-1. In animal models of diabetes, albiglutide administration stimulates increased β-cell mass. Following SC administration of a single 30-mg dose to patients with type 2 diabetes, maximum concentration is reached in 3-5 days with half-life of 3.6-6.8 days. The apparent volume of distribution after a single dose of albiglutide was 8.2-18.5 L. The eventual fate of albiglutide in the circulation is degradation into small peptides and individual amino acids. Albiglutide had no apparent effects on cardiovascular function, heart rate, electrocardiographic intervals, or respiratory function and did not produce any evidence of electrocardiographic abnormalities or arrhythmias in male cynomolgus monkeys. Furthermore, there were no albiglutide-related effects on neurobehavioral functional assessments. Albiglutide does not cross the blood–brain barrier to reach the satiety centers[1]. Albiglutide reduced myocardial infarct size and improved cardiac function and energetics following myocardial I/R injury which are associated with enhanced myocardial glucose uptake and a shift toward a more energetically favorable substrate metabolism by increasing both glucose and lactate oxidation[2].

プロトコル(参考用のみ)

動物実験 動物モデル Male Sprague-Dawley rats
投薬量 1, 3 or 10 mg/kg/day
投与方法 s.c.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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