Cyclosomatostatin
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。
Cas No.:84211-54-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。