标签归档：octreotide

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

发表于由

Octreotide acetate;(Synonyms: 醋酸奥曲肽; SMS 201-995 acetate) 纯度: 99.78%

Octreotide acetate是长效的天然生长抑素合成类似物，是比生长抑素更有效的生长激素，胰高血糖素和胰岛素的抑制剂。

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

Octreotide acetate Chemical Structure

CAS No. : 79517-01-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg) ; Apply now ;
10;mM;*;1 mL in DMSO ￥594 In-stock
10 mg ￥500 In-stock
50 mg ￥1116 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Octreotide acetate 相关产品

bull;相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Neuronal Signaling Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Peptidomimetic Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Macrocyclic Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Endocrinology Compound Library
  • NMPA-Approved Drug Library
  • Orally Active Compound Library
  • FDA Approved amp; Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library
  • Peptide Library

生物活性

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

体内研究
(In Vivo)

Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group[1]. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

1079.29

Formula

C51H70N10O12S2
CAS 号

79517-01-4
中文名称

醋酸奥曲肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:;

DMSO : ≥ 29 mg/mL (26.87 mM)

H2O : 25 mg/mL (23.16 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9265 mL 4.6327 mL 9.2654 mL
5 mM 0.1853 mL 0.9265 mL 1.8531 mL
10 mM 0.0927 mL 0.4633 mL 0.9265 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；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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

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：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.25 mg/mL (2.08 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (2.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.25 mg/mL (2.08 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (2.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.25 mg/mL (2.08 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (2.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Wang M, et al. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a month administration of octreotide. J Control Release. 2016 May 28;230:45-56.

    [2]. Kim S, et al. Treatment of Gastrin-Secreting Tumor With Sustained-Release Octreotide Acetate in a Dog. J Am Anim Hosp Assoc. 2015 Nov-Dec;51(6):407-12.
Animal Administration
[1]

Mice[1]
Thirty mice with HCC xenografts are randomLy divided into three groups: (A) Octreotide-soln group, (B) Octreotide-PPSG group, and (C) control group. Octreotide-soln group receives i.p. injection of 100 μg/kg octreotide-soln once a day and totally for consecutive 14 days. Octreotide-PPSG group receives a single subcutaneous injection of 1.4 mg/kg Octreotide-PPSG, and the injection volume is about 0.2 mL. Control group receives i.p. injection of saline once a day for consecutive 14 days. Treatment starts on the next day after injection of H22 hepatoma cell suspension and maintains for 14 days. Tumor growth is monitored by periodic caliper measurements on day 7 and day 14 post seeding. Tumor volumes (V) are calculated based on the length and width of tumor by Eq.
Rats[1]
Twelve male SD rats are divided into two groups, and housed in standard cages at 25°C, with free access to food and water for a week prior to the experiment. Rats are subcutaneously injected with Octreotidereotide solution (Octreotide-soln) or Octreotide-PPSG at an equivalent single dose of 20 mg/kg. The dose is determined based on the clinical dose of Octreotide-soln in human. Rats are fasted for 12 h before dosing and food is returned approximately 2 h post dosing. Blood samples are collected at predetermined time points using heparinized Eppendorf tubes. Immediately after collection, the blood samples are placed on ice until centrifuged at 3000 g for 10 min within 1 h. The plasma is collected and stored at −20°C until analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Wang M, et al. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a month administration of octreotide. J Control Release. 2016 May 28;230:45-56.

    [2]. Kim S, et al. Treatment of Gastrin-Secreting Tumor With Sustained-Release Octreotide Acetate in a Dog. J Am Anim Hosp Assoc. 2015 Nov-Dec;51(6):407-12.

Octreotide(Synonyms: 奥曲肽 SMS 201-995)

发表于由

Octreotide;(Synonyms: 奥曲肽; SMS 201-995) 纯度: 98.84%

Octreotide 是一种生长抑素类似物，能够与 somatostatin 受体结合，主要有 2，3，5 亚型，可增强 Gi 活性，降低胞内 cAMP 的产生。

Octreotideamp;;(Synonyms: 奥曲肽; SMS 201-995)

Octreotide Chemical Structure

CAS No. : 83150-76-9

规格 价格 是否有货 数量
1 mg ￥500 In-stock
5 mg ￥1200 In-stock
10 mg ￥2000 In-stock
25 mg ￥4000 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Octreotide 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Peptidomimetic Library
  • Peptide Library

生物活性

Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.

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].

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

1019.24

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

Protect from light

Powder -80deg;C 2 years
-20deg;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。
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

    [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.
Animal Administration
[2]

AMale PCK rats (n = 24) are assigned randomly to 1 of 4 groups (n = 6 per group): treatment by subcutaneous injection every 4 weeks treatment with 8 mg/kg Octreotide-LAR alone, 8 mg/kg PAS-LAR alone, co-application of 8 mg/kg Octreotide and 8 mg/kg PAS, or vehicle (microparticles liquid; CONT) from 4 to 16 weeks of age. The vehicle contains copolymer microparticles with polylactic-co-glycolic acid (PLGA). In 4- and 15-week-old conscious rats, heart rate (HR), diastolic blood pressure (DBP), and systolic blood pressure (SBP) are determined using a tail-cuff sphygmomanometer. Twenty-four-hour urine volume and food consumption are measured using metabolic cages after 15.5 weeks of age. After body weight measurement, the animals are anesthetized with sodium pentobarbital at 16 weeks of age, and the kidneys and liver are removed rapidly, causing lethal exsanguination. Total wet kidney weight and wet liver weight are measured, and blood samples are collected for measurements of serum urea nitrogen (SUN), aspartate amino transferase (AST), alanine aminotransferase (ALT), insulin-like growth factor-1 (IGF-1), glucose, insulin, glucagon, and cortisol.

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

    [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.