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Cyclosomatostatin Sale

目录号 : GC15495

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。

Cyclosomatostatin Chemical Structure

Cas No.:84211-54-1

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1mg
¥2,636.00
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 84211-54-1 SDF
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 SMILES O=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
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.2821 mL 6.4104 mL 12.8208 mL
5 mM 0.2564 mL 1.2821 mL 2.5642 mL
10 mM 0.1282 mL 0.641 mL 1.2821 mL
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