Octreotide Acetate; CAS 83150- 76 -9

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Product Description

Octreotide acetate;CAS 83150-76-9

Octreotide Acetate; CAS 83150-76-9
Octreotide acetate Chemical Properties
Boiling point  1447.2±65.0 °C(Predicted)
density  1.39±0.1 g/cm3(Predicted)
storage temp.  -20°C
solubility  H2O: soluble
pka 12.60±0.70(Predicted)
InChIKey DEQANNDTNATYII-MEUDYGGUSA-N
CAS DataBase Reference 83150-76-9
 
Safety Information
WGK Germany  3
 
MSDS Information
 
 
Octreotide acetate Usage And Synthesis
Description Octreotide is a long-acting somatostatin analog indicated for symptomatic control in acromegaly and gastroenteropancreatic tumors. Other potential uses under investigation include diabetes, psoriasis and Alzheimer's disease.
Originator Sandoz (Switzerland)
Uses Antisecretory (gastric).
Indications Octreotide acetate (Sandostatin) is a synthetic peptide analogue of the hormone somatostatin. Its actions include inhibition of the pituitary secretion of growth horm one and an inhibition of pancreatic islet cell secretion of insu lin and glucagon. Unlike somatostatin, which has a plasma half-life of a few minutes, octreotide has a plasma elimination half-life of 1 to 2 hours. Excretion of the drug is primarily renal.
Manufacturing Process Synthesis of octreotide and derivative thereof can be carried out by two methods. The first method is synthesized initially by fragment condensation solution phase procedures. The synthetic process of octreotide has been described by Ba uer et al. (1). The second method is the synthese by solidphase procedures. Edward et al. (2) isolated side chain protected octreotide with a total yield of 14% by cleaving the protected peptide from the resin with threoninol. Arano et al. (3) carried out another solid phase method for octreotide. and produced it in overall 31.8% yield based on the starting FmocThr(tBu)-ol-resin. The basic difference from the other procedures already described is that the introduction of the threoninol is carried out upon the protected peptidic structure (resin-free), which, when appropriately activated, leads quantitatively and without needing to make temporary protections upon the threoninol, to the protected precursor of octreotide, which in turn, with a simple acid treatment leads to octreotide with very high yields.
At first the Fmoc-Cys-Cl-trityl-resin was prepared. The incorporation of the Fmoc-Cys(trt)-OH residue upon 2Cl-Trt resin is accomplished with an excess of 1 eq. of Fmoc-Cys(Trt) and 2.5 eq. of N,N'-diisopropylethylamine (DIEA).
2.93 g (5.0 mmol) of Fmoc-Cys(Trt) are incorporated upon 5 g of resin (f = 1.28 mmol/g of resin, 6.4 mmol). The resin and the amino acid are weighed in separate containers and left to dry in a vacuum with KOH, for a minimum of two hours. A 1/1 solution of DIEA and CH2Cl2 (DCM) (dry on a 4A sieve) is prepared. The already dry amino acid is dissolved with dry DCM at a concentration of 0.1 g of resin per ml, adding the minimum quantity of dry DMF to complete the dissolution. 1/3 of the 1.8 ml (12.5 mmol) DIEA solution is added to this transparent solution in 1.8 ml of DCM. This is thoroughly homogenized and added to the dry resin. It is subjected to vigorous magnetic agitation for five minutes and the rest of the DIEA is added to the reaction; the mixture is allowed to react for forty minutes more. Then, 4 ml of dry MeOH are added and allowed to react for 10 minutes, after which the resin is filtered and the washings described below are carried out.
Brand name Sandostatin (Novartis).
Therapeutic Function Antiulcer, Growth horm one inhibitor
Biological Functions Octreotide acetate, a long-acting octapeptide analogue of somatostatin, has a half-life of approximately 100 minutes. A comparison of the primary structures of octreotide and somatostatin suggests little similarity, but from earlier work at the Salk Institute it was known that not all the residues in somatostatin were necessary to elicit its full biological activity. Other studies suggested that the essential fragment for its activity was the tetrapeptide Phe7-Trp8- Lys9-Thr10. These earlier studies helped in the design of the potent drug now known as octreotide acetate. This drug suppresses the secretion of gastroenteropancreatic peptides, such as gastrin, vasoactive intestinal peptide (VIP), insu lin, and glucagon, as well as pituitary GH. Furthermore, it is more potent than natural somatostatin in inhibiting the release of glucagon, in sulin, and GH.
Clinical Use Octreotide acetate is used by SC injection in the palliative treatment of patients with metastatic carcinoid tumors, which are tumors of the endocrine system, GI tract, and lung (gastroenteropancreatic). Carcinoid tumors secrete increasing amounts of vasoactive substances, including histamine, serotonin, bradykinin, and prostaglandins. Octreotide acetate inhibits or suppresses the release of these vasoactive substances and, thus, is useful in treating the severe diarrhea, facial flushing, and wheezing episodes that accompany carcinoid tumors. In addition, it finds use in the palliative management of VIP-secreting tumors (VIPomas, usually pancreatic tumors). Patients with VIPomas suffer a profuse, watery diarrhea syndrome, and octreotide acetate is able to help by decreasing the release of damaging intestinal tumor cell secretions. Octreotide also helps to reduce hypokalemia by correcting electrolyte imbalances.
An excessive secretion of GH from the pituitary can cause the disorder known as acromegaly, which is characterized by a progressive enlargement of the head, face, hands, feet, and thorax. Inasmuch as octreotide acetate is able to decrease the secretion of GH from the pituitary, it is used in treating patients with acromegaly who are unresponsive to previous pituitary radiation therapy or surgery. It is used in the treatment of acromegaly, because it reduces the blood levels of both GH and insulin-like growth factor-I (IGF-I). The long-acting repository form of octreotide acetate also is used in treating acromegaly, carcinoid tumors, and VIPomas, but in monthly depot injections.
Octreotide for IV injection is used in the treatment of acute bleeding from esophageal varices. Variceal bleeding occurs in about half the patients with cirrhosis of the liver and is responsible for about one-third of deaths in these patients. Octreotide is a potent vasoconstrictor that reduces portal and collateral blood flow by constricting visceral vessels, which leads to reduced portal blood pressure and decreases the bleeding.
Veterinary Drugs and Treatments Octreot ide may be useful in the adjunctive treatment of hyperins ulinemia in patients with insu linomas (especially dogs, ferrets). Response is variable, presumably dependent on whether the tumor cells have receptors for somatostatin. Octreotide may also be useful in the diagnosis and symptomatic treatment of gastrinomas in dogs or cats. It may be of use in the treatment of acute pancreatitis, but more research is needed before it can be recommended for this use in veterinary patients.
 
Octreotide Acetate; CAS 83150-76-9 Octreotide Acetate; CAS 83150-76-9 Octreotide Acetate; CAS 83150-76-9 Octreotide Acetate; CAS 83150-76-9
Company Informations:

Hunan Yunbang Pharmaceutical Co., Ltd. ( Yunbangpharm) located in Changsha High-tech Industrial Park, Hunan. It is a high-tech enterprise specializing in the research and development, production and sales of Pharmaceutical raw materials, Pharmaceutical intermediates(API) and Fine chemicals. Based in China, Yunbangpharm has been providing suitable solutions for many domestic,foreign pharmaceutical companies and traders. Excellent quality, good reputation and authentic price have won the praise of the majority of customers.
The company adheres to the corporate tenet of "We do not produce medicines, but help pharmaceutical companies make good medicines".

We can provide customers with customized processing, research and development services;
We can develop high-end Pharmaceutical and chemical products with high technical difficulties,high barriers and unique production processes;
We can provide 100 grams Grade, kilograms, and hundred kilograms of raw material pharmaceutical intermediates and other products.
We can perform -100°C to 300°C reaction.

R&D strength is the company's core competitiveness.Yunbangpharm has maintains a good cooperation relationship with many Universities and Research institutes locally, which can quickly transform R&D results into industrial production.

Our goal : To achieve the integrated upgrade of P harmaceutical intermediates, raw materials and high-end chemical products, adhere to "serving pharmaceutical companies, creating our brands" to provide customers with high-quality and low-cost pharmaceutical and chemical products, realizing Win-win cooperation and common development.

 

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