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Octreotide acetate

现货
Catalog No.
B4979
自身生长抑素的八肽同族物
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
10mg
¥ 400.00
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50mg
¥ 700.00
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Background

Octreotide acetate (Sandostatin) is an octapeptide congener of native somatostatin, inhibits the secretion of insulin and glucagon. It reduces production of IGF-1 and IGF-2 by the liver by modulation of growth-hormone secretion from the pituitary gland. [1]
The insulin-like growth factors IGF-1 and IGF-2, endogenously produced polypeptide hormones and potent stimulators of cell proliferation, are under investigation as clinical targets in prostate cancer.
Octreotide acetate decreased the urinary excretion of uric acid as well as the plasma concentrations of glucagon and insulin. Octreotide acetate decreased the urinary excretion of sodium and chloride without significiant influence on creatinine clearance, while the concentrations of lactic acid, pyruvic acid in blood, and cyclic AMP in plasma were not changed. [1]
References:
[1] Tetsuya yamamoto, Yuji moriwaki et al. Effect of Octreotide acetate on the Plasma Concentration and Urinary Excretion of Uridine and Purine Bases. Endocrine Journal 2002, 49(2),139-144.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1079.29
Cas No.83150-76-9
FormulaC51H70N10O12S2
SynonymsSMS 201995; Sandostatin
Solubility≥53.9645mg/mL in DMSO
Chemical Nameacetic acid;10-(4-aminobutyl)-19-[(2-amino-3-phenylpropanoyl)amino]-16-benzyl-N-(1,3-dihydroxybutan-2-yl)-7-(1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
SDFDownload SDF
Canonical SMILESCC(C1C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)NC(=O)C(CC5=CC=CC=C5)N)C(=O)NC(CO)C(C)O)O.CC(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人类HUV-EC-C内皮细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

1 μM, 72 hours

实验结果

与对照组培养物相比,1 nM Octreotide将细胞增殖减少45.8%,从9.7×103减少到4.4×103个细胞/孔。为了评估介质补充剂对HUV-EC-C细胞生长抑制的影响,针对培养基中的ECGF和肝素的分级浓度测试octreotide的效果。总之,与基线条件相比,这些变化没有显著影响octreotide的生长抑制活性。

动物实验 [2]:

动物模型

雄性Sprague-Dawley大鼠

给药剂量

皮下注射, 1 ?g/kg、10 ?g/kg和200 ?g/kg

实验结果

使用1 μg/kg octreotide处理后,NREMS和SWA均正常,但是,REMS在光照期显著增强。注射后2-3小时REMS开始增加,并在之后一天的时间中持续,尽管当考虑个体时间时它们的增加非常少。10 μg/kg octreotide注射后1小时内NREMS被显著抑制。计算12 h光照期,NREMS或SWA在基线和octreotide之间没有差异。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Danesi R, Agen C, Benelli U, et al. Inhibition of experimental angiogenesis by the somatostatin analogue octreotide acetate (SMS 201-995). Clinical Cancer Research, 1997, 3(2): 265-272.

[2] Beranek L, Obal Jr F, Taishi P, et al. Changes in rat sleep after single and repeated injections of the long-acting somatostatin analog octreotide. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 1997, 273(4): R1484-R1491.

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