Octreotide

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Octreotide

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。

CAS NO:

83150-76-9

奥曲肽
SMS 201-995

Octreotide (SMS 201-995) 是一种生长抑素受体 (somatostatin receptor) 激动剂，合成八肽生长抑素类似物。Octreotide (SMS 201-995) 可与生长抑素受体 (somatostatin receptor) 结合，主要有 2，3，5 亚型，可增强 Gi 活性，降低胞内 cAMP 的产生。具有抗肿瘤活性，可介导细胞凋亡 (apoptosis)，也可用于肢端肥大症的疾病研究。

生物活性

Octreotide (SMS 201-995) is asomatostatin receptoragonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to thesomatostatin receptorand mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediatesapoptosisand may also be used in disease studies in acromegaly^[1]^[2].

IC₅₀& Target

SSTR2

SSTR3

SSTR5

体外研究
(In Vitro)

Octreotide reverses the PA-induced alterations in Akt and GSK3β phosphorylation and expression of GS mRNA in HepG2 cells^[1]. Octreotide (10^-8mM, 6 hours) induces phosphorylated-glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity^[3].

Western Blot Analysis^[3]

Cell Line:	Human hepatoblastoma HepG2 cell line
Concentration:	10^-8mM
Incubation Time:	6 hours
Result:	Increased the protein expression levels of phosphorylated-Akt and GSK3β by 140.8% and 12.2%, respectively and the mRNA level of GS also increased.

体内研究
(In Vivo)

Octreotide significantly lowers the plasma glucose levels in the obese rats of the HFD group. Octreotide intervention significantly decreases the serum insulin concentration; however, there is no marked reduction in serum TG, TC, FFA, ALT and AST levels. Octreotide significantly inhibits the HOMA index. Octreotide decreases ipGTT and ipITT AUCs, but not significantly. Octreotide improves fat degeneration in rats with HFD-induced obesity and lipid droplet accumulation in PA-treated HepG2 cells. Octreotide promotes the phosphorylation of Akt and GSK3β and the expression of GS mRNA in rats with HFD-induced obesity^[1]. Octreotide reduces body weight and wet kidney weight compared with the vehicle-treated (CONT) group. PAS and Octreotide/PAS treatment decrease cAMP levels, but Octreotide alone does not in PCK rats. In the Octreotide/PAS group, there are a significantly fewer pS6-positive cells than in the PAS alone group^[2].

Clinical Trial

分子量

1019.24

性状

Solid

Formula

C₄₉H₆₆N₁₀O₁₀S₂

CAS 号

83150-76-9

Sequence

Phe-Cys-Phe-Trp-Lys-Thr-Cys-Thr (Disulfide bridge: Cys2-Cys7)

Sequence Shortening

FCFWKTCT (Disulfide bridge: Cys2-Cys7)

中文名称

奥曲肽

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据

In Vitro:

H₂O : 100 mg/mL(98.11 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	0.9811 mL	4.9056 mL	9.8112 mL
5 mM	0.1962 mL	0.9811 mL	1.9622 mL
10 mM	0.0981 mL	0.4906 mL	0.9811 mL

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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (98.11 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。