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Cyclosomatostatin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cyclosomatostatin图片
CAS NO:84211-54-1
包装:1mg
市场价:2636元

产品介绍
Cyclosomatostatin 是一种有效的生长抑素 (SST) 受体拮抗剂。 Cycloomatostatin 可以抑制 1 型生长抑素受体 (SSTR1) 信号传导并减少结直肠癌 (CRC) 细胞中的细胞增殖、ALDH+ 细胞群大小和球体形成。
Cas No.84211-54-1
化学名(3S,6R,9S,12S)-9-((1H-indol-3-yl)methyl)-6-(4-aminobutyl)-12-benzyl-3-((R)-1-(benzyloxy)ethyl)-1,4,7,10,13-pentaazacycloicosane-2,5,8,11,14-pentaone
Canonical SMILESO=C([C@@H](CCCCN)NC([C@H](CC1=CNC2=CC=CC=C12)NC([C@H](CC3=CC=CC=C3)NC4=O)=O)=O)N[C@H](C(NCCCCCC4)=O)[C@@H](C)OCC5=CC=CC=C5
分子式C44H57N7O6
分子量779.98
溶解度Soluble to 1 mg/ml in 20% ethanol / Water
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: N/A

Cyclosomatostatin is a non-selective somatostatin receptor antagonist.

Somatostatin is a regulatory hormone or tissue factor playing an inhibitory role in the normal regulation of several organ systems including hypothalamus and pituitary gland, central nervous system, gastrointestinal tract as well as pancreas.

In vitro: Although cyclosomatostatin could fully block the effect of somatostatin, it only partially reversed the inhibitory effect of cortistatin, a new anti-inflammatory peptide. This observation was further supported by the fact that cyclosomatostatin reversed the antiinfl ammatory effect of somatostatin and octreotide in vitro completely, while only partially reversing the effect of cortistatin [1].

In vivo: The effect of cortistatin was found to be dose dependent, with dose as low as 0.5 nmol (50 μg/kg) being partially protective. In contrast, cyclosomatostatin, somatostatin as well as octreotide were not protective [1].

Clinical trial: As the precursor of cyclosomatostatin, somatostatin has already been introduced in the clinical practice in some macrophage populations. Somatostatin shows protective effect in certain inflammatory disorders including pancreatitis and liver injury. However, somatostatin is not protective in lethal septic shock [1].

Reference:
[1] Gonzalez-Rey E,Chorny A,Robledo G,Delgado M.  Cortistatin, a new antiinflammatory peptide with therapeutic effect on lethal endotoxemia. J Exp Med.2006 Mar 20;203(3):563-71.