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Octreotide acetate 83150-76-9 OXTREOTIDE
Octreotide acetate
CAS: 83150-76-9
Molecular Formula: C49H66N10O10S2
Molecular Formula | C49H66N10O10S2 |
Molar Mass | 1019.24 |
Density | 1.39±0.1 g/cm3(Predicted) |
Melting Point | >140°C (dec.) |
Boling Point | 1447.2±65.0 °C(Predicted) |
Flash Point | 829.053°C |
Solubility | Soluble in acetic acid, DMSO, and methanol |
Vapor Presure | 0mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
pKa | 12.60±0.70(Predicted) |
Storage Condition | -20°C |
Stability | Hygroscopic |
Refractive Index | 1.673 |
Physical and Chemical Properties | [Α] D20-42 °(C = 0.5,95% acetic acid). |
Use | Can inhibit growth hormone, inhibit gastrointestinal pancreas secretion of polypeptides somatostatin analogs in the treatment of acute esophageal venous hemorrhage and acromegaly. |
WGK Germany | 3 |
Reference
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1. Cai Zhiyuan Wang tangles Guo Huailiang et al. Effects of two chemical drugs on behavior and physiology of plateau zok... |
peptide drugs | Novartis Sandostatin (octreotide acetate), is a synthetic natural somatostatin octapeptide derivatives, it retains a pharmacological effect similar to that of somatostatin, and the effect is long-lasting. Indications for octreotide acetate include acromegaly; Alleviation of symptoms and signs associated with functional gastroenteropancreatic endocrine neoplasia; And efficacy in Carcinoid Tumors presenting with carcinoid syndrome, VIP tumors, and glucagon tumors. In addition, octreotide acetate for gastrinomas/Zollinger-Ellison syndrome (usually in combination with proton pump inhibitors or H2 receptor blockers), Insulinomas (preoperative prevention of hypoglycemia and maintenance of normal blood sugar), the effective rate of growth hormone releasing factor tumor is about 50%. Novartis had global sales of $1.4 billion. In the Chinese market, in 1999 by Novartis began to import sales, in addition, India Sun Pharmaceutical Co., Ltd. also began to import sales in 2009. More than 20 domestic products are on the market. In 0.183 billion, the use of octreotide acetate in sample hospitals in 16 key cities in China reached RMB 52.77%, with Novartis accounting for half of the total, reaching. |
indication | octreotide acetate is a national health insurance Class B drug, which is a synthetic natural octapeptide derivative of somatostatin, compared with natural somatostatin, the half-life of somatostatin is obviously prolonged and has the same pharmacological effects, including inhibition of growth hormone function, inhibition of gastric acid, pancreatic enzyme, glucagon and insulin secretion, and reduction of visceral blood flow, decreased gastrointestinal motility. Compared with native somatostatin, octreotide has a long half-life, is more selective for inhibition of growth hormone secretion than for inhibition of insulin secretion, and does not cause rebound hypersecretion of the hormone. 1, control surgery or radiation therapy can not adequately control the disease in patients with acromegaly symptoms and reduce the patient's growth hormone (GH) insulin-like growth factor -1(1GF-1) plasma levels. Sandostatin may also be used to treat patients with acromegaly who are unable or unwilling to undergo surgery, or to treat patients with acromegaly who have not yet had radiation therapy. 2. Alleviation of symptoms associated with functional gastroenteropancreatic (GEP) endocrine tumors such as carcinoid tumors with carcinoid syndrome manifestations. Sandostatin is not an anti-cancer drug and does not cure these patients. 3, prevention of complications after pancreatic surgery. 4, liver cirrhosis patients with gastric-esophageal variceal bleeding caused by emergency treatment, hemostasis and prevention of rebleeding, Sandostatin should be combined with endoscopic sclerotherapy and other special treatment. |
Use | The effect is similar to that of natural endogenous somatostatin, and the effect is strong and lasting. It is used to relieve the symptoms caused by tumors of the stomach, intestine, pancreatic endocrine system or carcinoid tumors, and has no effect on the treatment of tumors. can inhibit growth hormone, inhibit gastrointestinal pancreas secretion of polypeptide |
production method | compound (I) is hydrogenated first, debenzylating the protecting group, and then (II) in dimethylformamide, the compound (III) was obtained by coupling dicyclohexylcarbodiimide (DCC) with HOBt. (Iii) demethylation of the Benzyl protecting group by hydrogenation, followed by interaction of DCC and HOBt in dimethylformamide, and coupling with (IV) gives (V). (V) reacts with hydrazine and is converted to (VI). Further coupling of (VII) and (viii) gives (IX). (Ix) after removal of the tert-butyl protecting group, (X) is coupled with (VI) to give (X). (X) reacted with trifluoroacetic acid, thioanisole, Tris (trifluoroacetic acid) boron and trifluoroacetic acid successively to remove the protecting group, and finally oxidized by air to obtain octreotide. |
Mol Download Chemical properties
CAS:
83150-76-9
MF:
C49H66N10O10S2
MW:
1019.24
EINECS:
1533716-785-6
MDL No.:
MFCD07780622
Melting point:
>140°C (dec.)
Boiling point:
1447.2±65.0 °C(Predicted)
Density
1.39±0.1 g/cm3(Predicted)
storage temp.
-20°C
solubility
Soluble in acetic acid, DMSO, and methanol
pka
12.60±0.70(Predicted)
form
Solid
color
White to Off-White
Water Solubility
Soluble to 1.20 mg/ml in water
Stability:
Hygroscopic
InChIKey
DEQANNDTNATYII-MEUDYGGUSA-N
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