Octreotide acetate|83150-76-9|(奥曲肽; SMS 201-995)-陌孚医药/Medlife

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Octreotide acetate (Synonyms: 奥曲肽; SMS 201-995)

目录号: PC10788 纯度: ≥98%

CAS No. :83150-76-9

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中文名称

Octreotide acetate

中文别名

醋酸奥曲肽;[R-(R^<*>^,R^<*>^)]-D-苯丙酰-L-半胱氨酰-L-苯丙酰-D-色胺酰-L-赖氨酰-1-苏氨酰-N-[2-羟基-1-(羟基甲基)丙基]-L-苏氨酰胺环(2→7)二硫化物;醋酸奥曲肽 OCTREOTIDEACETATE;▲醋酸奥曲肽;奥曲肽;奥曲肽标准品;醋酸奥曲肽 Octreotide Acetate;[R-(R^^,R^^)]-D-苯丙酰-L-半胱氨酰-L-苯丙酰-D-色胺酰-L-赖氨酰-1-苏氨酰-N-[2-羟基-1-(羟基甲基)丙基]-L-苏氨酰胺环(2→7)二硫化物;[R-(R^<*>^,R^<*>^)]-D-苯丙酰-L-半胱氨酰-L-苯丙酰-D-色胺酰-L-赖氨酰-1-苏氨酰-N-[2-羟基-1-(羟基甲基)丙基]-L-苏氨酰胺环(2 →7)二硫化

英文名称

Octreotide acetate

英文别名

Octreotide acetate;L-cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-(2-hydroxy-1-(hydroxymethyl) propyl)-cyclic (2->7)-disulfide, (R-(R*,R*));Sandostatin;Sms 201-995;(4R,7S,10S,13R,16S,19R)-13-((1H-Indol-3-yl)methyl)-19-((R)-2-amino-3-phenylpropanamido)-10-(4-aminobutyl)-16-benzyl-N-(1,3-dihydroxybutan-2-yl)-7-((R)-1-hydrox;Octreotide;ctreotide;DARAMONOL;D-Phe-Cys(1)-Phe-D-Trp-Lys-Thr-Cys(1)-N-[(1R,2R)-1-(Hydroxymethyl)-2-hydroxypropyl]-NH2;H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-L-threoninol acetate salt (Disulfide bond);Longastatin;Ocetreotide,Acetate;OCTREOTIDE ACETATE (GMP);Octreotode Acetate;OXTREOTIDE;Phe-c(Cys-Phe-Trp-Lys-Thr-Cys)-CH(CH2OH)-CH(OH)-CH3;Sandostatin<*>;[R-(R*,R*)]-D-Phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[2-hydroxy-1-(hydroxy-methyl)propyl]-cysteinamide cyclic(2->7)-disulfide;7)-disulfide

Cas No.

83150-76-9

分子式

C₄₉H₆₆N₁₀O₁₀S₂^.₂(C₂H₄O

分子量

1139.35

包装储存

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。

生物活性

Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

性状

Solid

IC50 & Target[1][2]

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. Octreotide (10mM, 6 hours) induces phosphorylated?glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	Human hepatoblastoma HepG2 cell line
Concentration:	10mM
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. 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

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。

ClinicalTrial

SequenceShortening

FCFWKTCT (Disulfide bridge: Cys2-Cys7)

Sequence

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

参考文献

[1]. Wang XX, et al. Effects of octreotide on hepatic glycogenesis in rats with high fat diet?induced obesity. Mol Med Rep. 2017 Jul;16(1):109-118 [Information]

[2]. Kugita M, et al. Beneficial effect of combined treatment with octreotide and pasireotide in PCK rats, an orthologous model of human autosomal recessive polycystic kidney disease. PLoS One. 2017 May 18;12(5):e0177934. [Information]

[3]. Xiao-Xia Wang,et al. Effects of octreotide on hepatic glycogenesis in rats with high fat diet?induced obesity. Mol Med Rep. 2017 Jul;16(1):109-118. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

建议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溶液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (98.11 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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