Xi`an Eastling Biotech Co., Ltd.
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CAS NO.79517-01-4
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C51H70N10O12S2 |
| Molar Mass | 1079.3 |
| Melting Point | 153-156°C |
| Boling Point | 1447.2°C at 760 mmHg |
| Specific Rotation(α) | D20 -42° (c = 0.5 in 95% acetic acid) |
| Flash Point | 829.1°C |
| Solubility | H2O: soluble |
| Vapor Presure | 0mmHg at 25°C |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| In vivo study | 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. 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. |
usage and dosage for the treatment of VIP tumor, carcinoid syndrome and gastrinoma. Insulinoma and glucagonoma, 50 ~ lOOug subcutaneous injection every time, 1~2 times a day, can be maintained by intermittent medication after symptom relief. It can also be used to treat acromegaly caused by growth hormone releasing factor (GHF) tumor. In the treatment of gastrointestinal disease fistula, Diarrhea, cirrhosis of the liver and portal hypertension and esophageal variceal bleeding, gastric ulcer disease bleeding, acute pancreatitis.
Last Update：2022-01-01 11:11:39
Open Data Verified Data
side effects were Abdominal Pain, abdominal distension, Diarrhea, steatorrhea; Gallstone formation; Glucose tolerance may decrease or worsen in the early stage of treatment, and then improve; No endogenous antibody production in long-term use, there was no obvious rebound or adverse reaction when the drug was stopped and rapidly reduced. The remainder was octreotide acetate.
Last Update：2022-01-01 11:11:39
| digestive system drugs | octreotide is a kind of digestive system drugs, which is a synthetic octapeptide cyclic compound, it is a homolog of natural Somatostatin, has the pharmacological activity of natural Somatostatin, and has a long-term effect (the half-life of this product is 1.5 hours, while the natural Somatostatin is 2~3 minutes). This product has a selective inhibitory effect on the secretion of growth hormone, glucagon and insulin, and has a stronger effect than natural somatostatin. Animal experiments have proved that: intravenous injection of this product for 15 minutes, the inhibitory effect on the release of growth hormone is 70 times that of natural somatostatin, and the inhibition of insulin is 3 times that of natural somatostatin. It also has inhibitory effects on thyrotropin, adrenocorticotropic hormone, gastrin, cholecystokinin and vasoactive intestinal polypeptide, and can inhibit the secretion of gastric acid, pancreatic amylase, lipase and pepsin. It can slow down the passage time of gastrointestinal tract, promote the absorption of water and electrolyte, has a constrictive effect on visceral blood vessels, can reduce visceral blood flow and liver blood flow, so as to reduce Portal pulse pressure and portal blood flow, reduces intestinal hypersecretion and may enhance intestinal absorption of water and Na +. The 1, 4 and 8 amino acids in the chemical structure of this product are non-natural amino acids, so they are not easily destroyed by enzymes and have a long half-life. Subcutaneous injection of this product is absorbed quickly and completely, the peak time of blood drug concentration is 0.5 hours, the distribution volume is 0.27L/kg, the half-life is 1.5 hours, the metabolic clearance rate is 160ml/min. It was biphasic eliminated by intravenous injection, and half-life of α-phase and β-phase was 10 minutes and 90 minutes, respectively. The plasma protein binding rate was 65%. clinically, octreotide is mainly used to treat esophageal varices, acromegaly, gastrointestinal bleeding caused by portal hypertension, such as liver cirrhosis, esophageal varices bleeding, peptic ulcer bleeding and Stress ulcer bleeding, pancreatic diseases such as severe acute pancreatitis, pancreatic fistula after pancreatic injury or surgery, and prevention of complications after pancreatic surgery. Also used for gastrointestinal fistula, digestive endocrine tumors such as intestinal vasoactive peptide tumor, gastrinoma, glucagonoma, Ectopic ACTH syndrome, carcinoid syndrome, acromegaly, exophthalmos hyperthyroidism, persistent, refractory following total colectomy Diarrhea and AIDS-related Diarrhea. Intrathecal injection can treat cancer pain. |
| usage and dosage | (1) prevention of complications after pancreatic surgery: 1 hour before surgery, subcutaneous injection of 0.1mg octreotide; after 0.1mg subcutaneous injection, 3 times a day, for 7 days. (2) treatment of esophageal variceal bleeding caused by Portal Hypertension: intravenous injection of 0.1mg, then 0.5mg, every 2 hours 1 intravenous drip. (3) Stress ulcer and gastrointestinal bleeding: 0.1mg subcutaneous injection, 3 times a day. (4) severe pancreatitis: 0.1mg subcutaneous injection, 4 times a day, 3~7 days of treatment; Pancreatic injury or postoperative pancreatic fistula, subcutaneous injection, 0.1mg each time, 1 times every 8 hours, 7~14 days. (5) Gastrointestinal tract fistula and gastrointestinal endocrine system tumor adjuvant therapy: subcutaneous injection of 0.1mg, 3 times a day, a course of 10 to 14 days. (6) digestive system endocrine tumor, Graves' disease, Acromegaly and AIDS-related Diarrhea: subcutaneous injection of 0.1mg, 3 times a day, acromegaly treatment for 10 to 14 days. After the use of the main injection site pain or acupuncture, generally in 15 minutes to relieve. gastrointestinal adverse reactions included anorexia, Nausea, Vomit, Diarrhea, abdominal spasm pain, etc, impaired glucose tolerance and abnormal liver function (increased gamma-glutamyltransferase and slightly increased transaminase). Kidney, pancreatic dysfunction and cholelithiasis patients with caution. Pregnant women, lactating women and children are contraindicated. |
| biological activity | octretide acetate is a long-acting synthetic analog of natural somatostatin, which is a more effective growth hormone than somatostatin, inhibitors of glucagon and insulin. |
| category | toxic substances |
| toxicity grade | high toxicity |
| Acute toxicity | intravenous-rat LD50: 18.1 mg/kg; Intravenous-mouse LD50: 72.3 mg/kg |
| flammability hazard characteristics | flammable; Decomposition of toxic nitrogen oxides, sulfur oxides smoke |
CAS:
79517-01-4
MF:
C51H70N10O12S2
MW:
1079.3
EINECS:
616-695-4
MDL No.:
MFCD08277638
Melting point:
153-156°C
alpha
D20 -42° (c = 0.5 in 95% acetic acid)
storage temp.
Inert atmosphere,Store in freezer, under -20°C
solubility
H2O: soluble
form
Solid
color
White to Off-White
Stability:
Hygroscopic
InChIKey
XQEJFZYLWPSJOV-XJQYZYIXSA-N
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.