Vapreotide Acetate

Vapreotide Acetate
Details:
1.General Specification(in stock)
(1)API(Pure powder)
(1)Injection
2.Customization:
We will negotiate individually, OEM/ODM, No brand, for secience researching only.
Internal Code: KP-3-78/002
Vapreotide CAS 103222-11-3
Molecular formula: C57H70N12O9S2
HS Code: /
Molecular weight: 1131.37
EINECS number: 253-368-1
MDL No.: MFCD30489723
Main market: USA, Australia, Brazil, Japan, Germany, Indonesia, UK, New Zealand , Canada etc.
Analysis: HPLC, LC-MS, HNMR
Technology support: R&D Dept.-3
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Description
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Vapreotide acetate is an artificially synthesized octapeptide somatostatin analogue with a unique cyclic structure, composed of specific amino acid sequences connected by peptide bonds, and containing a pair of disulfide bonds, which endows it with high molecular stability and specific biological activity. Its molecular formula is C57H70N12O9S2, and its molecular weight is 1131.37.

 

It has demonstrated extensive application value in clinical practice. It has high affinity for somatostatin receptor subtypes SSTR-2 and SSTR-5, effectively treating acute esophageal variceal bleeding by inhibiting the release of vasoactive peptides and reducing portal vein pressure, and preventing recurrence of bleeding after endoscopic treatment. In addition, it is also used to treat gastrointestinal bleeding, acromegaly, pancreatitis and other diseases, and has a certain tumor suppressive effect on neuroendocrine tumors and prostate cancer.

 
Our Products Description
 
Vapreotide Acetate | Shaanxi BLOOM Tech Co., Ltd
Vapreotide | Shaanxi BLOOM Tech Co., Ltd
Vapreotide | Shaanxi BLOOM Tech Co., Ltd

Vapreotide acetate Price List | Shaanxi BLOOM Tech Co., Ltd

Vapreotide acetate Price List | Shaanxi BLOOM Tech Co., Ltd

 Method of Analysis | Shaanxi BLOOM Tech Co., Ltd

Vapreotide COA

  Shaanxi BLOOM Tech Co., Ltd
Certificate of Analysis
Compound name Vapreotide
Grade Pharmaceutical grade
CAS No. 103222-11-3
Quantity 55g
Packaging standard PE bag+Al foil bag
Manufacturer Shaanxi BLOOM TECH Co., Ltd
Lot No. 202601090078
MFG Jan 9th 2026
EXP Jan 8th 2029
Structure

Vapreotide acetate structure | Shaanxi BLOOM Tech Co., Ltd

Item Enterprise standard Analysis result
Appearance White or almost white powder Conformed
Water content ≤5.0% 0.54%
Loss on drying ≤1.0% 0.42%
Heavy Metals Pb≤0.5ppm N.D.
As≤0.5ppm N.D.
Hg≤0.5ppm N.D.
Cd≤0.5ppm N.D.
Purity (HPLC) ≥99.0% 99.98%
Single impurity <0.8% 0.52%
Total microbial count ≤750cfu/g 95
E. Coli ≤2MPN/g N.D.
Salmonella N.D. N.D.
Ethanol (by GC) ≤5000ppm 500ppm
Storage

Store in a sealed, dark, and dry place below -20°C

Vapreotide acetate NMR | Shaanxi BLOOM Tech Co., Ltd

 Shaanxi BLOOM Tech Co., Ltd

Chemical Formula C57H72N12O9S2
Exact Mass 1132
Molecular Weight 1133
m/z 1132 (100.0%), 1134 (61.6%), 1135 (18.7%), 1134 (9.0%), 1135 (5.6%), 1133 (4.4%), 1136 (3.7%), 1134 (2.7%), 1135 (1.8%), 1137 (1.7%), 1133 (1.6%), 1136 (1.1%)
Elemental Analysis C, 60.40; H, 6.40; N, 14.83; O, 12.70; S, 5.66

 Usage | Shaanxi BLOOM Tech Co., Ltd

Vapreotide acetate signaling route | Shaanxi BLOOM Tech Co., Ltd

Inhibition of adenylate cyclase and cAMP signaling route

After binding to the receptor, the Gi protein mediated signaling route inhibits adenylate cyclase activity, thereby reducing intracellular cyclic adenosine monophosphate (cAMP) levels. CAMP, as an important second messenger, plays a crucial role in regulating various cellular functions, and its concentration changes directly affect the activity of downstream molecules such as protein kinase A (PKA). By reducing cAMP concentration, PKA activity decreases, thereby inhibiting various cellular responses that rely on this route. This framework not only affects the secretion process, but also participates in cellular metabolic regulation and signal integration. In addition, a decrease in cAMP levels can alter ion channel activity and gene transcription processes, leading to a lower overall cellular activity. Therefore, inhibition of the cAMP signaling route constitutes an important mechanistic basis for the regulation of various physiological processes by vasopressin.

Inhibition framework of hormone secretion related signaling routes

In various endocrine genes, vapreotide acetate works together through multiple signaling routes to inhibit hormone secretion related processes. This framework mainly involves the coordinated regulation of multiple links such as cAMP reduction, calcium ion influx reduction, and membrane potential change. Through these changes, the formation, transport, and release of cellular secretory granules are inhibited. In addition, vasopressin can also affect protein expression and vesicle fusion frameworks related to secretion, thereby regulating the secretion process at multiple levels. This framework has high integration and does not rely on a single signal path, but achieves overall suppression effect through the joint action of multiple routes. Therefore, its framework in regulating secretion related physiological processes is complex and systematic.

Vapreotide acetate framework | Shaanxi BLOOM Tech Co., Ltd
Vapreotide acetate cell | Shaanxi BLOOM Tech Co., Ltd

Regulatory framework of cell proliferation and apoptosis related routes

At the cellular level, the process of gene proliferation and apoptosis can also be influenced by regulating relevant signaling routes. Research has shown that it affects gene cycle progression by inhibiting key signaling networks such as MAPK (mitogen activated protein kinase) route and PI3K/Akt route. In addition, it can further affect gene expression patterns by regulating intracellular calcium signaling and transcription factor activity. These changes work together to decrease the rate of gene proliferation and promote apoptosis related processes under certain conditions. This framework reflects its profound impact on gene growth regulation and is an important component of its molecular action network.

The integration framework of neuroendocrine regulatory network

The framework of action in the neuroendocrine system is reflected in the integrated regulation of complex regulatory networks. In this system, multiple signaling molecules and feedback loops participate in the regulation process together. By acting on multiple key nodes and affecting the signal transmission path, the overall network activity is altered. In addition, it can further enhance the regulatory effect by regulating the interaction between central and peripheral signals. This multi-level and multi node operation mode gives it strong integration ability in complex regulation systems. Therefore, its framework is not limited to a single route, but manifests as a systemic impact on the entire network.

Vapreotide acetate network | Shaanxi BLOOM Tech Co., Ltd
Vapreotide acetate action | Shaanxi BLOOM Tech Co., Ltd

Receptor desensitization and regulatory framework

In the process of sustained action, receptor desensitization and regulatory frameworks are also involved. As receptors are activated for a long time, genes may reduce their sensitivity to signals through receptor endocytosis, phosphorylation, and degradation. This process helps prevent excessive signal activation and maintain system stability. In addition, the receptor recycling process also participates in regulation, allowing genes to adjust their response capabilities at different time scales. This framework reflects the adaptive regulation of cgenes to external signals and is an important factor in maintaining long-term homeostasis. Therefore, receptor desensitization and re regulation frameworks constitute an indispensable part of its action process.

The overall framework characteristics of multi-channel collaborative regulation

Overall, the framework of action of vapreotide acetate does not rely on a single signaling route, but rather achieves overall regulation through the synergistic action of multiple frameworks. These frameworks include receptor binding, regulation of second messengers, changes in ion channels, and integration of cellular signaling networks at multiple levels. In the actual physiological environment, these frameworks are intertwined and jointly determine their ultimate effects. In addition, the relative importance of these frameworks may vary among different tissues and gene types, resulting in diverse regulatory patterns. Therefore, the framework of action is highly complex and systematic, and is a typical representative of multi route synergistic effects.

Vapreotide acetate uses | Shaanxi BLOOM Tech Co., Ltd
Vapreotide acetate influence | Shaanxi BLOOM Tech Co., Ltd

The framework of influence on signals related to hemodynamic regulation

The framework of hemodynamic regulation is mainly reflected in the regulation of vascular related signaling routes. By acting on receptors on vascular smooth muscle genes and endothelial genels, it can affect intracellular signaling processes and regulate vascular tension. In this process, the decrease of cAMP and changes in ion channels jointly participate, causing changes in the contractile state of vascular smooth muscle genes. In addition, indirect frameworks can also affect the distribution of local blood flow, leading to an overall adjustment in the hemodynamic state. This framework involves the integrated regulation of multiple signaling routes and exhibits certain differences in different tissues. Therefore, its impact on hemodynamics exhibits multi-level regulatory characteristics.

Discovering History

1970s: The discovery and research of somatostatin laid the foundation

The origin of the development of vasopressin acetate can be traced back to the discovery of somatostatin in the 1970s.

 

In 1973, researchers first isolated this peptide hormone with broad inhibitory functions from the hypothalamus and found that it could regulate various endocrine and exocrine processes. This discovery quickly attracted widespread attention and prompted in-depth research on its structure, receptors, and functions. However, due to the extremely short half-life and poor stability of natural somatostatin in vivo, its direct application is limited. 

In the early 1980s, the development of somatostatin analogs was initiated

In the 1980s, with the development of peptide synthesis technology, researchers began to systematically design and screen somatostatin analogs to improve their stability and pharmacokinetic properties. At this stage, multiple analogs with cyclic structures or key amino acid modifications were developed, including octreotide, which later became a representative drug, and early structural prototypes of vapreotide acetate. The research focuses on improving receptor selectivity, prolonging half-life, and enhancing in vivo stability. 

Mid to late 1980s: Stage of structural optimization and pharmacological research

In the mid to late 1980s, as a new type of somatostatin analogue, it entered the stage of systematic research. Researchers have modified amino acid sequences to significantly improve stability while maintaining biological activity.

 

The research in this stage mainly focuses on in vitro receptor binding experiments and pharmacological property evaluation in animal models. The results indicate that it exhibits stable and controllable regulatory effects in multiple physiological regulatory systems. 

Early 1990s: Entering the clinical research stage

In the early 1990s, it began to enter the clinical research stage. Early clinical trials mainly evaluate its safety, tolerability, and basic pharmacological characteristics. At this stage, researchers gradually clarify its functional characteristics in the human body and conduct preliminary exploration of its manifestations in different pathological states. Meanwhile, comparative studies with other somatostatin analogs are gradually being conducted to evaluate their relative advantages in clinical applications. 

Mid to late 1990s: Exploration and positioning of clinical applications

In the mid to late 1990s, with the deepening of clinical research, application positioning gradually formed in specific fields. Multiple studies have evaluated its performance in complex pathological states and further clarified its role in the comprehensive treatment system. At the same time, its comparative studies with other similar drugs are constantly increasing, making its advantages and limitations gradually clear. 

 

At the beginning of the 21st century: competition with other similar substances and adjustment of application scope

After entering the 21st century, with the widespread application of somatostatin analogs such as octreotide and lanreotide, it faces a more intense competitive environment. In this context, its application scope has gradually been adjusted, focusing more on specific fields. At the same time, researchers have also begun to reassess its advantages in different clinical scenarios and explore its potential value in combination therapy. In addition, the emergence of the new generation of long-acting formulations has also had a certain impact on their development, causing a change in their position in the pharmaceutical system. 

2010s: Research gradually decreases but still has reference value

In the 2010s, the number of new studies on it gradually decreased, partly due to the emergence of a new generation of drugs. However, the large amount of data accumulated in previous studies still has important reference value, especially in understanding the overall mode of action of somatostatin analogs. In addition, its research results as a classical molecule are still widely cited and play a role in teaching and basic research. At this stage, vapreotide acetate is regarded as one of the representative drugs with historical significance, and its development process has become an important case in the research of peptide drugs.

References

 

1. Patel Y.C. Somatostatin and its receptor family. Frontiers in Neuroendocrinology, 1999.

2. Lamberts S.W.J., van der Lely A.J., de Herder W.W., Hofland L.J. Octreotide. New England Journal of Medicine, 1996.

3. Reisine T., Bell G.I. Molecular biology of somatostatin receptors. Endocrine Reviews, 1995.

4. Hoyer D., et al. Somatostatin receptors. Pharmacological Reviews, 1995.

5. Bruns C., et al. Somatostatin receptor subtypes and signal transduction. Metabolism, 1996.

6. Oberg K. Neuroendocrine tumors: molecular mechanisms. Annals of Oncology, 2004.

7. Saltz L., et al. Vapreotide and somatostatin analogues in cancer therapy. Cancer Research, 1993.

 

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