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Octreotide Powder CAS 79517-01-4
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Octreotide Powder CAS 79517-01-4

Octreotide Powder CAS 79517-01-4

Product Code: BM-2-4-049
CAS number: 79517-01-4
Molecular formula: C51H70N10O12S2
Molecular weight: 1079.3
EINECS number: 616-695-4
MDL No.: MFCD08277638
Hs code: 2937190000
Analysis items: HPLC>99.0%, LC-MS
Main market: USA, Australia, Brazil, Japan, Germany, Indonesia, UK, New Zealand , Canada etc.
Manufacturer: BLOOM TECH Changzhou Factory
Technology service: R&D Dept.-4
Usage: Pure API(Active pharmaceutical ingredient) for science research only
Shipping: Shipping as another no sensitive chemical compound name

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Octreotide Powder is an artificially synthesized somatostatin analogue (molecular formula: C₄₉H₆₆N₁₀O₁₀S₂), existing in the form of a white to off-white lyophilized powder. It should be stored in a dark place and refrigerated at 2-8℃. As a long-acting octapeptide derivative, its pharmacological effect is 30 times stronger than that of natural somatostatin, with a half-life extended to 90-120 minutes (naturally only 2-3 minutes). It works by inhibiting the secretion of hormones such as growth hormone (GH), insulin, glucagon, and 5-hydroxytryptamine.
Main applications:
Endocrine tumors: Acromegaly (GH inhibition), Neuroendocrine tumors (such as carcinoid syndrome);
Gastrointestinal bleeding: Emergency hemostasis for rupture of esophageal varices;
Rare disease: Long-term management of congenital hyperinsulinism.
Usage Note: It should be re-suspended in a sterile state before subcutaneous or intravenous injection. Common side effects include gastrointestinal discomfort, blood sugar fluctuations, and the risk of gallstones. The powder form is convenient for precise preparation, but strict adherence to GMP standards is required. Currently, it is a commonly used peptide preparation in clinical settings, and its use for non-medical purposes is illegal.

Customized Bottle Caps & Corks

 

 

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Applications

 

Octreotide powder is an artificially synthesized octapeptide analogue belonging to the class of somatostatin analogues. It plays a therapeutic role in various diseases by inhibiting the pathological secretion of peptides in the gastrointestinal and pancreatic endocrine systems.  It uses of octreotide for gi bleed is very common, injection how to give is something we have to be concerned about.  Uses of it infusion is widely and indications, injection uses we have to pay attention to from time to time.

  • Prevention of complications after pancreatic surgery

After pancreatic surgery, complications such as pancreatic fistula and bleeding can be prevented.

Prevention and therapy of gastric and esophageal variceal bleeding: can be used to prevent and treat gastric and esophageal variceal bleeding, reducing the risk of re bleeding.

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Octreotide uses | Shaanxi BLOOM Tech Co., Ltd
  • The therapy of acromegaly

It can be used for the therapy of acromegaly, especially for patients with residual or recurrent symptoms after surgery and radiation therapy. It can effectively control the related symptoms of acromegaly, such as headaches, visual field defects, etc.

Relief of functional islet cell carcinoma: It can alleviate symptoms and signs related to functional islet cell carcinoma, such as hypoglycemia, hyperinsulinemia, etc.

  • Adjuvant therapy for liver diseases

It can be used as an adjuvant therapy for liver diseases such as hepatitis and cirrhosis, helping to reduce portal pressure and alleviate related symptoms.

  • Conservative therapy of intussusception

In some cases, it can also be used for conservative therapy of intussusception, by inhibiting the secretion of digestive fluid, allowing the part of the intussusception to have the opportunity to self reduce

Octreotide uses | Shaanxi BLOOM Tech Co., Ltd
Octreotide uses | Shaanxi BLOOM Tech Co., Ltd
  • Research on anti-tumor activity

It has anti-tumor activity and can mediate cell apoptosis, which helps to study the mechanisms of tumor occurrence and development. In the laboratory, it can be used for in vitro and in vivo anti-tumor experiments to explore its inhibitory effect on tumor cell growth.

  • Growth hormone related research

commonly used in the laboratory to study the secretion and regulation of growth hormone. It can inhibit the release of growth hormone, which helps to gain a deeper understanding of the physiological and pathological effects of growth hormone.

  • Drug screening and development

As a somatostatin analogue, it can be used for drug screening and development. By studying the interaction with the target, new drug molecules with potential therapeutic effects can be discovered, further promoting the development process of new drugs.

  • Cell culture and experimental model establishment

It can be used in the laboratory to establish cell culture models and experimental animal models to study their mechanisms of action in various disease states. By using processed cell or animal models, disease processes can be simulated to gain a deeper understanding of the pathogenesis and potential therapeutic strategies of diseases.

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Manufacturing Information

 

The laboratory synthesis of octreotide powder typically uses the Solid Phase Peptide Synthesis (SPPS) method. This method uses amino resin on a solid-phase carrier as the starting material, and constructs a peptide chain by sequentially adding the required amino acid residues.

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Solid phase carrier selection

Choose a suitable solid phase carrier for peptide synthesis, commonly used carriers include styrene polymers and polyvinyl alcohol. Fix the amino resin on the carrier to form a solid-phase synthetic resin.

Side chain allyl protection

In some cases, in order to prevent side chain allyl reactions during the synthesis process, allyl protection is necessary. Common protective groups include trifluoroacetyl and chloroacetyl groups.

Deprotection of side chain allyl groups

After completing the cyclization reaction on the desired amino acid residue, the reaction of deprotection of side chain allyl groups is carried out. Usually, acid or alkaline solutions are used for deprotection operations.

Condensation of amino resin

The required amino acids are condensed with amino resin to form the first amino acid residue of the peptide chain. The condensation reaction usually uses dichloromethane as the solvent, N-hydroxysuccinimide (NHS) and 1- (3-Dimethylaminopropyl) -3-ethylcarbodiimide (EDC) as coupling agents.

R-CHOCO-NH-R + R-NH + NHS + C2H4Cl2 → R-CHOCO-NH-R + NHS + C2H4Cl2

Cyclization reaction

Transforming linear peptide chains into cyclic structures is one of the key steps in the synthesis of it. Cyclization can be achieved through different methods, such as forming ester bonds, amide bonds, etc. The commonly used cyclization method is to connect one end of the peptide chain to the other end, forming a circular structure.

Cutting and purification

Cut peptide chains from solid-phase carriers and purify them to remove unreacted raw materials and by-products. Common cutting reagents include TFA (trifluoroacetic acid) or HCl, etc. Purification is usually achieved through column chromatography or crystallization.

Quality testing and control

The synthesized is subjected to quality testing and control through analytical methods such as mass spectrometry and high-performance liquid chromatography to ensure that its purity and quality meet the requirements.

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Other properties

 

This drug, as a highly specific and artificially synthesized octapeptide somatostatin analogue, has shown broad application prospects and significant therapeutic effects in the field of clinical medicine since its inception. It not only inherits the core pharmacological properties of natural somatostatin, but also enhances its biological activity and stability through subtle structural adjustments and optimizations, making it play an irreplaceable role in the therapy of various diseases related to endocrine and exocrine pancreatic dysfunction.

Pharmacological mechanism of octreotide

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Inhibit endocrine and pancreatic secretion

Endocrine pancreas, mainly composed of pancreatic islet cells, is responsible for secreting various hormones, among which insulin and glucagon are key factors in regulating blood glucose balance. it can selectively bind to somatostatin receptors on pancreatic cell membranes by mimicking the mechanism of action of somatostatin, activating a series of signaling pathways and ultimately inhibiting insulin secretion by pancreatic beta cells and glucagon secretion by pancreatic alpha cells. This process is particularly important for the therapy of diabetes and its complications, because excessive insulin secretion can aggravate insulin resistance, and the abnormal rise of glucagon will lead to difficult control of blood sugar levels. The intervention of it helps to restore the balance of pancreatic function and promote blood glucose stability.

Inhibit the release of bicarbonate and digestive enzymes from exocrine pancreas

The exocrine pancreas is mainly composed of acinar cells and ductal cells, responsible for secreting pancreatic juice, which contains a large amount of bicarbonate and various digestive enzymes (such as trypsin, pancreatic lipase, pancreatic amylase, etc.), which are crucial for the digestion and absorption of food. However, in certain pathological conditions, such as acute pancreatitis, acute exacerbation of chronic pancreatitis, etc., excessive secretion of pancreatic juice and activation of digestive enzymes can trigger self digestion of pancreatic tissue, leading to severe inflammatory reactions and tissue damage. It reduces the release of bicarbonate and digestive enzymes by inhibiting the secretion activity of acinar cells, thereby alleviating the self digestion burden of the pancreas and protecting pancreatic tissue from further damage. This mechanism of action makes this one of the preferred drugs for treating acute pancreatitis and preventing its recurrence.

Octreotide 250mcg | Shaanxi BLOOM Tech Co., Ltd

Clinical application of octreotide powder

Adjuvant therapy for gastrointestinal bleeding

 

 

It also has a certain vasoconstrictive effect, which can reduce visceral blood flow, thereby lowering portal vein pressure and reducing the risk of esophageal and gastric variceal bleeding. Therefore, in the therapy of liver cirrhosis combined with esophageal and gastric variceal bleeding, it is often used as an adjuvant therapy drug, combined with endoscopic therapy, triple lumen double balloon tube compression and other methods to improve the success rate of hemostasis.

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Therapy of acute pancreatitis

Acute pancreatitis is a disease of the pancreas caused by the self digestion of trypsin. Its onset is sudden, the condition is dangerous, and the mortality rate is high. This has become an important drug in the therapy of acute pancreatitis by inhibiting pancreatic exocrine secretion, reducing the stimulation and damage of pancreatic juice to pancreatic tissue, and alleviating systemic inflammatory response. Research has shown that early application of it can significantly reduce the incidence of complications and mortality in acute pancreatitis, and improve the prognosis of patients.

Adjuvant treatment for chronic pancreatitis

Patients with chronic pancreatitis often experience recurrent abdominal pain, pancreatic endocrine dysfunction, and other symptoms. Through its inhibitory effect on pancreatic exocrine secretion, can alleviate abdominal pain symptoms caused by excessive secretion of pancreatic juice in patients, while also helping to protect pancreatic tissue and delay disease progression. In addition, it can improve pancreatic endocrine function and promote insulin secretion and utilization, which is particularly applicable to chronic pancreatitis patients with diabetes.

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This is a long‑acting synthetic octapeptide analog that mimics the biological actions of endogenous somatostatin but exhibits significantly improved metabolic stability and prolonged pharmacological activity. It acts as a selective agonist for somatostatin receptors, with high affinity for subtypes 2, 3, and 5, which are widely distributed in tissues such as the brain, hypothalamus, pituitary gland, pancreas, and gastrointestinal tract.

Upon binding to these receptors, it activates inhibitory Gi protein‑coupled signaling pathways, reduces intracellular cyclic adenosine monophosphate (cAMP) concentrations, and subsequently suppresses abnormal cell proliferation and excessive hormone secretion, making it highly effective in managing hormone‑driven disorders. Beyond its well‑established use in acromegaly, it plays a critical role in alleviating life‑altering symptoms caused by various neuroendocrine tumors, including carcinoid tumors and vasoactive intestinal peptide‑secreting (VIP) tumors.

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Octreotide Price | Shaanxi BLOOM Tech Co., Ltd

These neoplasms often release large quantities of bioactive substances that trigger severe watery diarrhea, cutaneous flushing, abdominal cramps, and electrolyte disturbances.By strongly inhibiting the hypersecretion of these pathogenic hormones, it effectively relieves symptoms, improves nutritional status, and enhances patients' quality of life. Clinically, this medicine is available in multiple formulations, including immediate‑release injectable solutions for acute management and long‑acting depot injections for sustained therapeutic control, enabling personalized dosing schedules that adapt to different disease conditions and patient requirements.

Although mild gastrointestinal adverse reactions such as abdominal pain, nausea, diarrhea, and flatulence may occur during initial therapy, these effects are usually transient and well‑tolerated with continued use. Due to its highly specific receptor‑targeting mechanism and reliable clinical efficacy, it remains an indispensable therapeutic agent for diseases involving hormone overproduction and uncontrolled cellular growth. Ongoing clinical studies continue to explore its expanded applications, including potential uses in inflammatory disorders, certain types of cancer, and other conditions where somatostatin signaling may provide therapeutic benefits.

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