H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH
somatostatin
CAS: 38916-34-6;51110-01-1
Molecular Formula: C76H104N18O19S2
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Names and Identifiers
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Physico-chemical Properties
| Molecular Formula | C76H104N18O19S2 |
| Molar Mass | 1637.88 |
| Density | 1.43±0.1 g/cm3(Predicted) |
| Melting Point | >211°C (dec.) |
| Boling Point | 1970.9±65.0 °C(Predicted) |
| Flash Point | 1145.7°C |
| Water Solubility | Soluble in water(25,00°C 1,00 g/L), Methanol. |
| Solubility | H2O: 1mg/mL |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | powder |
| Color | White to Off-White |
| Merck | 13,8788 |
| BRN | 6436064 |
| pKa | 2.94±0.70(Predicted) |
| Storage Condition | −20°C |
| Refractive Index | 1.669 |
| MDL | MFCD00076762 |
| Use | Treatment of low blood pressure and other symptoms |
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Risk and Safety
| WGK Germany | 3 |
| RTECS | WF8751700 |
| FLUKA BRAND F CODES | 3-10-21 |
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Nature
Open Data Verified Data
- This product is a hypothalamic polypeptide hormone, containing a disulfide bond of the tetradecapeptide, can be secreted by the central nerve cells, islet cells and gastrointestinal tract D cells, with a wide range of inhibitory effects: inhibiting the release of growth hormone; Inhibiting the release of thyroid stimulating hormone; Inhibiting the secretion and release of prolactin; Inhibiting the secretion of insulin and glucagon; Inhibiting the secretion of calcitonin and inhibiting the secretion of renin; for some acromegaly patients can inhibit the secretion of corticotropin; Inhibit the secretion of digestive hormones and digestive juice; Reduce visceral blood flow, as well as the role of nerve.
- This product is lack of species specificity, and is easy to cause rebound after drug withdrawal. The aging period is very short, only 1~3min for normal people, and 5 min for patients with liver and kidney. Applications are limited. Somatostatin in plasma of patients with somatostatin tumor can be as high as normal 250 times.
Last Update：2024-01-02 23:10:35
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Standard
Authoritative Data Verified Data
This product is a chemically synthesized cyclic polypeptide consisting of fourteen amino acids, and has the same structure as the hypothalamic hormone that inhibits the release of human growth hormone. According to the water, no acetic acid calculation, containing somatostatin ((C76H104N18019S2) should be 95.0% ~ 104.0%.
Last Update：2024-01-02 23:10:35
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Trait
Authoritative Data Verified Data
- This product is white or off-white powder.
- This product is soluble in water, almost insoluble in dichloromethane, and soluble in 1% acetic acid solution.
specific rotation
take this product, precision weighing, add acetic acid solution to dissolve and quantitatively dilute the solution containing about 2mg per lml, according to the law (General 0621), according to the water, without acetic acid, the specific rotation was -37 ° to -47 °.
Last Update：2022-01-01 11:39:05
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.611 ml | 3.053 ml | 6.105 ml |
| 5 mM | 0.122 ml | 0.611 ml | 1.221 ml |
| 10 mM | 0.061 ml | 0.305 ml | 0.611 ml |
| 5 mM | 0.012 ml | 0.061 ml | 0.122 ml |
Last Update：2024-01-02 23:10:35
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Use
Open Data Verified Data
- treatment of acromegaly caused by hypersecretion of growth hormone, middle-aged and elderly diabetes. It is also used to treat glucagon hypersecretory islet a cell tumor, gastrinoma of gastrointestinal tract D cells or islet a cells, and to treat gastric ulcer bleeding.
- usage and dosage of intravenous drip above lOOug.
Last Update：2022-01-01 11:11:38
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Differential diagnosis
Authoritative Data Verified Data
- take an appropriate amount of this product and the reference substance of somatostatin, respectively add water to dissolve and dilute to prepare a solution containing 1 mg per 1 ml. According to the thin layer chromatography (General 0502) test, absorb the above two solutions of 10 u1, respectively, on the same silica gel G thin layer plate, with glacial acetic acid-pyridine-water-n-butanol (10:15:20:45) as a developing solvent, it was developed, dried with hot air, sprayed with 0.1% ninhydrin ethanol solution, and heated at 115 ° C. For about 5 minutes until spots appeared. The position and color of the main spot displayed by the test solution should be the same as the position and color of the main spot of the reference solution.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
Last Update：2022-01-01 11:39:05
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Exam
Authoritative Data Verified Data
amino acid ratio
take this product, add 6mol/L hydrochloric acid solution, at 110 ° C after 24 hours of hydrolysis, according to the appropriate amino acid analysis method. Using 1/8 of the total number of moles of aspartic acid, alanine, lysine, glycine and phenylalanine as 1 to calculate the relative ratio of each amino acid, the following provisions shall be met: 0.90-1.10 of aspartic acid, glycine 0.90~1.10, alanine 0.90~1.10, phenylalanine 2.7~3.3, serine 0.7~1.05, threonine 1.4~2.1, cysteine 1.4~2.1, lysine 1.8~2.2.
acidity
Take 10mg of this product, Add 10ml of water to dissolve, and then measure it according to law (General rule 0631). The pH value should be 4.5~6.5.
absorbance
take this product, precision weighing, plus 0.9% sodium chloride solution to dissolve and quantitatively dilute into a solution containing 0.05mg per lml, according to UV-visible spectrophotometry (General 0401) determination, the absorbance at a wavelength of 280nm must not be greater than 0.20.
acetic acid
take about 15mg of this product, weigh it accurately, put it in A 10ml measuring flask, add diluent [mobile phase A (General 0872)-methanol (95:5)] to dissolve and dilute to the scale, shake well, as a test solution, according to the determination method of acetic acid in synthetic polypeptide (General 0872), the content of acetic acid should be 3.0% ~ 15.0%.
Related substances
take this product, add water to dissolve and dilute to make a solution containing 0.5mg per lml as a test solution; Take 2ml for precision measurement, put it in a 100ml measuring flask, dilute it with water to the scale, as a control solution. According to the determination of high performance liquid chromatography (General rule 0512), silica gel was bonded with eighteen alkyl silane as filler; Phosphoric acid solution (11ml of phosphoric acid was taken, ml of water was added, and the pH value was adjusted to 2.3 with triethylamine, diluted to 1000ml with water) as mobile phase A, acetonitrile as mobile phase B; Flow rate of 1.5ml per minute; Detection wavelength of 215nm; Gradient elution was carried out as follows. Take about 10mg of somatostatin control, put it in a 20ml measuring flask, add 1ml of 30% hydrogen peroxide solution, place it for 1 hour, dilute it with water, shake it well, filter it, and take the filtrate 50 u1, note human liquid chromatograph, the number of theoretical plates is not less than 2000 according to the calculation of somatostatin peak, and the separation degree of somatostatin peak and the peak of oxidative degradation product with relative retention time of about 1.1 should be not less than 2.0. The sample solution and the control solution are respectively 50 u1, and the human liquid chromatograph is injected respectively, and the chromatogram is recorded. If there are impurity peaks in the chromatogram of the test solution, except for the solvent peak, the area of a single impurity peak shall not be greater than 0.5 times (1.0%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (2.0%).
moisture
take this product, according to the determination of moisture (General 0832 first method), the water content shall not exceed 8.0%.
bacterial endotoxin
take this product, check according to law (General 1143), each 1 mg of somatostatin containing endotoxin should be less than 30EU.
Last Update：2022-01-01 11:39:06
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Content determination
Authoritative Data Verified Data
determined by HPLC (General 0512)
chromatographic conditions and system suitability test
silica gel was bonded with octylsilane as filler; Phosphoric acid solution (11ml of phosphoric acid was taken, water was added to 2.3 ML, pH was adjusted to with triethylamine, and diluted to ML with water)-acetonitrile (75:25) as mobile phase; The flow rate was 1.5ml per minute; The detection wavelength was 215nm. The number of theoretical plates was not less than 1500 according to the somatostatin peak.
assay
take an appropriate amount of this product, weigh it accurately, add water to dissolve and quantitatively dilute it to make it contain 0.lmg solution, as the test solution, the precision of 20ul injection liquid chromatograph, record the chromatogram; The appropriate amount of somatostatin control, the same method for determination. According to the external standard method to calculate the peak area, that is.
Last Update：2022-01-01 11:39:07
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Category
Authoritative Data Verified Data
pituitary hormone release inhibitory drugs.
Last Update：2022-01-01 11:39:07
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Storage
Authoritative Data Verified Data
shading, sealing, storage in cold place.
Last Update：2022-01-01 11:39:07
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Somatostatin for injection
Authoritative Data Verified Data
This product is a sterile freeze-dried product made of somatostatin and appropriate excipients, containing somatostatin (C76H104N18019S2) should be 90.0% to 110.0% of the label amount.
trait
This product is white or off-white loose lumps or powder.
identification
- take this product, add water to dissolve and dilute to make a solution containing about 1 mg per 1ml, take 1ml, and add 1ml of Alkaline copper tartrate test solution, which shows blue purple.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
examination
- acidity take this product, add water to dissolve and dilute to make a solution containing 0.5mg per lml, mix well, and measure according to law (General rule 0631). The pH value should be 4.5~6.5.
- clarity and color of solution take this product, add water to dissolve and dilute to make a solution containing 0.5mg per 1 ml, the solution should be clear and colorless; If it is turbid, it shall not be more concentrated than the turbidity standard liquid No. 1 (General rule 0902 method 1); In case of color development, it shall not be deeper than the yellow Standard Colorimetric liquid No. 1 (General rule 0901 method 1).
- Related substances take this product, according to the method under the item of somatostatin inspection, should comply with the provisions.
- The content uniformity shall be calculated according to the content of each bottle measured under the content determination item, and shall comply with the regulations (General rule 0941).
- the moisture content of this product shall not exceed 0832 as determined by the method for determination of moisture (General rule 4.0% first method).
- abnormal toxicity take this product, add sodium chloride injection to dissolve and dilute to make a solution containing 0.5mg per lml, and check according to law (General rule 1141), should comply with the provisions.
- the bacterial endotoxin is taken from this product and checked according to law (General rule 1143). The amount of endotoxin contained in somatostatin per 1 mg should be less than 30EU.
- sterile take this product, with pH 7.0 sterile sodium chloride-peptone buffer solution after the appropriate amount of membrane filtration treatment, with Staphylococcus aureus as positive control bacteria, according to law inspection (General 1101), the requirements shall be met.
- others should comply with the relevant provisions under injection (General 0102).
Content determination
Take 10 bottles of this product and add appropriate amount of water respectively to dissolve and quantitatively dilute the contents to make about 0. A solution of 1 mg was obtained as a test solution by measurement according to the method described under somatostatin.
category
Same as somatostatin.
specification
(1)0.25mg (2)0.75mg (3)2mg (4)3mg
storage
light shielding, closed, stored in cold place.
Last Update：2022-01-01 11:39:08
H-ALA-GLY-CYS-LYS-ASN-PHE-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH - Reference Information
| overview | somatostatin acetate, that is, growth hormone release inhibitory factor, is an endogenous regulatory hormone existing in the human body and has a wide range of physiological functions Inhibitory effect. Somatostatin English name: Somatostatin, molecular formula: C76H104N18O19S2, molecular weight 1637.89. Somatostatin is synthesized from the median uplift of the hypothalamus and delta cells of the islets. It was isolated from the hypothalamus of sheep by Dr. Guillemin of Germany in 1973 and its structure was elucidated. For this reason, Dr. Guillemin won the Nobel Prize in Medicine and Physiology in 1977. The chemical structure of somatostatin is a tetradecapeptide with a pair of disulfide bonds in the molecule. It mainly exists in the central nervous system and surrounding organs (such as: stomach, intestine, pancreas, skin, etc.) in the human body. The maximum concentration is the following thalamus, but the digestive tract has the largest content. It is often used clinically for severe acute esophageal variceal bleeding, severe acute gastric and duodenal ulcer bleeding, acute erosive gastritis or hemorrhagic gastritis, adjuvant treatment of pancreas, gallbladder and intestine, and adjuvant treatment of diabetic ketoacidosis. Other roles and uses are being discovered with the deepening of its basic research and clinical practice. Therefore, the application prospect of somatostatin is broad, and the market demand is increasing year by year. |
| application | somatostatin acetate is often clinically used in severe acute esophageal variceal bleeding, severe acute gastric and duodenal ulcer bleeding, acute erosive gastritis or hemorrhagic gastritis, adjuvant treatment of pancreas, gallbladder and intestine, adjuvant treatment of diabetic ketoacidosis. |
| mechanism of action | somatostatin acetate exerts its diversity and specificity through endocrine, exocrine, neurogenic secretion and special paracrine. It has inhibitory effects on growth hormone, thyrotropin, insulin, glucagon, pancreatic polypeptide, cholecystokinin, gastrin and other hormones. It can also inhibit gastric acid and liver bile secretion, affecting gastrointestinal absorption, movement and blood flow. It has a protective effect on pancreatic, liver and stomach cells. |
| physiological function | 1. inhibit the secretion of growth hormone, prolactin, thyrotropin and adrenocorticotropic hormone from the pituitary gland. 2. Inhibit the secretion of insulin, glucagon, vasoactive intestinal peptide, pancreatic polypeptide, gastrin, cholecystokinin and motilin by endocrine cells of pancreas and gastrointestinal tract. 3. Inhibit the secretion of pancreatic juice bicarbonate, pancreatic enzymes, water, gastric acid, hematopoietic factors, pepsin, etc. from the pancreas and gastrointestinal exocrine glands. 4. Inhibit gastrointestinal motility and absorption of glucose, amino acids and triglycerides, and promote ion transport. 5. Inhibit visceral blood flow. 6. Inhibit cell proliferation and tumor growth. 7. Adaptive protective effect on gastric mucosal cells and liver cells. 8. Inhibit CNS activity. 9. Activate opiate receptors. 10. Inhibit or stimulate histamine release. |
| pharmacokinetics | t1/2 is 1.1~3min after intravenous injection, t1/2 for liver disease patients is 1.2~8min after injection, and t1/2 for chronic renal insufficiency patients is 2.6~4.9min after injection. The product was dropped at a speed of 75 μg/h, reaching a stable concentration of 1250 μg/L within 15min, with a metabolic clearance rate of about 1L/min and t1/2 of 2.7min. This product is rapidly metabolized in liver, mainly excreted in urine, excreted in 40% after 4 hours and 70% after 24 hours. Clinically, it is mainly used for upper gastrointestinal bleeding caused by various reasons, especially esophageal-gastric varices; it is also used for adjuvant treatment of pancreatic, biliary, and intestinal fistulas; prevention and treatment of complications of pancreatic surgery; diabetic acidosis Adjuvant treatment; also used for the treatment of acromegaly and its complications. |
| usage and dosage | acute severe upper gastrointestinal hemorrhage: continuous intravenous drip at a speed of 250 μg/h; If necessary, 250 μg is injected intravenously for not less than 3min. After hemostasis, the drug was administered continuously for 48~72h, and the total course of treatment was not more than 120h. Prevention of postoperative complications of pancreatitis: intravenous drip at the beginning of the operation at a speed of 250 μg/h until the 5th day after operation. Acute pancreatitis: intravenous drip at 250 μg/h for 5~7 days. Diabetic ketoacidosis: intravenous drip at a speed of 100~500 μg/h; At the same time combined with insulin therapy. |
| attention and taboos | during continuous intravenous administration, continuous drip should be carried out, and the dressing change time should not exceed 1min. If the interruption time is long, 250 μg of impact should be given again, followed by drip at a speed of 250 μg/h. If it is possible to use an infusion pump for administration to obtain a stable input. This product is not suitable for arterial bleeding. Treatment of acute pancreatitis should be administered immediately after diagnosis. Injecting this product can cause transient nausea, red face, abdominal pain, diarrhea and mild changes in blood sugar. This product should be kept at a low temperature of 2~8 ℃. |
Last Update：2024-04-10 22:40:09
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Product Name: somatostatin Request for quotation
CAS: 38916-34-6
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CAS: 38916-34-6
Tel: 17505222756
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