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CAS NO.50-56-6
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C43H66N12O12S2 |
| Molar Mass | 1007.19 |
| Density | 1.1086 (rough estimate) |
| Melting Point | 192-194°C |
| Boling Point | 1533.3°C at 760 mmHg |
| Specific Rotation(α) | D22 -26.2° (c = 0.53) |
| Flash Point | 881.1°C |
| Water Solubility | Soluble in water. |
| Solubility | Very soluble in water. It dissolves in dilute solutions of acetic acid and of ethanol (96 per cent). |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | lyophilized powder |
| Color | White |
| Merck | 13,7049 |
| BRN | 3586108 |
| pKa | pKa ～6.1(free amino group on Cys) (Occasionally);～10(free phenol on Tyr) (Occasionally) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.6700 (estimate) |
| Physical and Chemical Properties | White to yellow-brown powder, hygroscopic, soluble in water. |
| Use | Uterotonic drugs |
| uterine contractile drug | oxytocin, also known as oxytocin, is a seed uterine contractile drug that can be extracted or chemically synthesized from the posterior lobe of the pituitary gland of animals. The chemically synthesized product does not contain vasopressin, has no pressor effect, has selective excitation effect on uterine smooth muscle, and strengthens its contraction. The uterus in labor is most sensitive to oxytocin (increased estrogen secretion), the immature uterus is not reactive to this product. The reactivity of the uterus to oxytocin in the early or second trimester of pregnancy is low, and it gradually increases in the late pregnancy, reaching the highest before labor. Small doses can strengthen the rhythmic contraction of the smooth muscle at the bottom of the uterus, strengthen its contractility, accelerate the frequency of contraction, and the nature of contraction is similar to natural childbirth, and maintain polarity and symmetry, so it is clinically used for induced labor and induced labor. Large doses make the uterine muscles contract ankylosing. It is clinically used to compress the blood vessels between muscle fibers, prevent postpartum hemorrhage and postpartum involution, and promote lactation, shrink the breast ducts, and promote the discharge of milk from the breast, but it cannot increase The secretion of milk can only promote milk excretion. It should be noted that the dosage and drip speed should be strictly controlled when used for induced labor or induced labor, so as not to cause tonic uterine contraction, resulting in fetal asphyxia death or uterine rupture. If there is no cephalopelvic, fetal position or other birth canal abnormalities, contraindicated, poor uterine contraction, history of cesarean section and more than 3 times of maternal contraindicated. Oxytocin preparations extracted from the pituitary gland of cattle and pigs occasionally cause allergic reactions, and intravenous drip too fast can cause mild vasodilation and blood pressure drop. The fastest dripping speed does not exceed 40~60 drops per minute. A slightly larger dose is also used for postpartum hemorrhage, fetal clothing, etc. In recent years, it has been found that this product has a good effect on pulmonary hemoptysis, and has a good effect on gastrointestinal function relaxation after vagus nerve resection or abdominal surgery. oral administration is ineffective and easy to be destroyed by digestive juice, but it can be absorbed by oral mucosa. intravenous drip of 0.01 IU can cause physiological contraction of uterus (rhythmic, polar and symmetrical) within 1-3 minutes, and the holding time is short, with a half-life of only 2.5-3 minutes and a large dose of myotonic contraction of uterine muscle. It has a synergistic effect with prostaglandins. Oxytocin is often combined with ergot preparations to treat postpartum hemorrhage; abortion is inevitable; it is mainly used for induction of labor in late pregnancy and delayed labor caused by uterine atony during labor; used for oxytocin sensitivity test; used for oxytocin irritation Test; assist postpartum milk discharge; hemoptysis; postoperative gastrointestinal motility delay. |
| biological activity | Oxytocin (α-Hypophamine; Oxytocic hormone) is a multi-effect hypothalamic peptide (hypothalamic peptide) that helps childbirth, breastfeeding and prosocial behavior. Oxytocin can be used as a stress response molecule with anti-inflammatory, antioxidant and protective effects, especially in the face of adversity or trauma. |
| Animal Model: | Fifty-six male Lister-hooded rats (150-200 g) |
| Dosage: | 0.1 mg/kg-0.3 mg/kg |
| Administration: | Subcutaneousinjection; 0.1 mg/kg-0.3 mg/kg; single dose |
| Result: | Produced significantly greater hypothermia (at 0.3 mg/kg) than the saline group. |
| use | this product can be absorbed from oral mucosa and selectively act on uterine smooth muscle to promote uterine contraction. Suitable for birth and labor retardation. The effect is the same as that of oxytocin after intravenous drip. For pelvic stenosis, a history of uterine surgery (including caesarean section), excessive labor pains, obstruction of the birth canal, placental abruption, severe pregnancy poisoning maternal contraindicated. Uterine contractile drugs. Used for induced labor, induced labor, postpartum and after abortion due to uterine contraction weakness caused by uterine bleeding. Nose drops can promote milk discharge. Adverse reactions and contraindications: during delivery, obvious cephalopelvic disproportion, umbilical cord exposure or prolapse, complete placenta previa, too narrow pelvis, and too strong uterine contraction are prohibited. Placental abruption, heart disease, oversized uterus, pregnant women over 35 years old, history of caesarean section, history of myomectomy and breech delivery should be used with caution. With oxytocin in sacral block, severe hypertension and even cerebrovascular rupture can occur. It cannot be injected in the same solution with norepinephrine. There are incompatibility with hydrolyzed protein. |
| production method | method 1. extraction method (currently used in our country, the purity is low, but the cost is low) extraction of oxytocin solution 100g of leaf dry powder and 30g of quartz powder are put into a ball mill, distilled water is added, and the same method is used for extraction four times. The amount of distilled water added was 1.4L twice and 1.3L twice. Each extraction for 45min, centrifugation, liquid collection, residue extraction. Merge four extracts to obtain oxytocin solution. After leaf dry powder [water, ball mill] → chromatography separation of oxytocin extract 1500g of pre-treated artificial zeolite, adding 20L of 0.25% acetic acid solution, stirring and pouring into an exchange column, adding the extract when the acetic acid solution drops to 2-3cm above the surface of zeolite, and collecting white turbid solution at an appropriate flow rate (mainly containing oxytocin, because of its pI7.7, while vasopressin pI10.9 is easy to become a positive ion and is adsorbed). When the liquid level of the extract drops to the surface of the zeolite, immediately add distilled water and continue to collect the turbid liquid until it runs out. The turbid liquid was adjusted to 3.5 with glacial acetic acid, heated to 95 ℃ in a water bath for 3min, cooled quickly and refrigerated overnight. Oxytocin extract [HAc, artificial zeolite column] → turbid solution [HAc, heating] → adsorption and elution of the separation solution the next day, the refrigerated solution is filtered, the filtrate is added with 10% bentonite slurry (3ml per 100ml) under stirring, adsorption for 1h, centrifugation. The supernatant was checked with sulfosalicylic acid test solution, and no precipitation occurred for complete adsorption. If it is not complete, it is adsorbed again and precipitated twice. The bentonite is eluted four times with 1% acetic acid (1.6L, 1.4L, 1.2L and 0.8L respectively). When the eluate is heated to 80 ℃, trichlorotert-butanol is added, the temperature is raised to 95 ℃, the temperature is quickly cooled to 25 ℃, the filtrate is filtered or centrifuged, the filtrate is combined four times, and the titer and vasopressin limit are detected. Cold storage solution [filtration] → filtrate [bentonite slurry] → adsorbate [1% HAc]→ preparation of eluate oxytocin injection the measured qualified oxytocin solution is diluted to 5U/ml or 10U/ml, filtered by No. 4 or No. 5 vertical melting funnel, potted, and sterilized by circulating steam at 100 ℃ for 30min to obtain the finished product. Oxytocin solution (qualified for determination) [filter potting, sterilization] → Oxytocin injection. Note: After the artificial zeolite treats the new boiling stone through a 60-80 mesh sieve, add 2L of distilled water every 500g, adjust sodium hydroxide to pH9, keep it for half an hour, pour out the supernatant, add 2L of water, adjust to pH9, pour out the supernatant, add water, stir and add dilute sulfuric acid to lower the pH to 5.8-6, stir for half an hour, pour out the supernatant, and then use child water every time, repeatedly wash 7-8 times. Add 1L of water and dilute sulfuric acid, stir for half an hour, pour out the supernatant, wash with water to pH7, filter to dry, and dry for later use. Regeneration of Artificial Zeolite Wash artificial zeolite twice with distilled water, then add 1.5L of water (calculated by zeolite 500g) and 150g of sodium chloride to stir for 2 hours, wash to remove vasopressin, and then wash with distilled water until there is no chloride ion. Add a proper amount of water, adjust the pH to 9 with sodium hydroxide, stir for half an hour, pour out the supernatant, wash with distilled water, adjust the pH to 5.5-6 with sulfuric acid, then wash with water to near neutral, filter dry, and dry at 105 ℃ for later use. Add appropriate amount of water before use, adjust with glacial acetic acid, stir and soak. The preparation of 10% bentonite slurry is mixed according to the volume ratio of bentonite mass to water of 1:10, grinding for about 1h, and adjusting pH with acetic acid in grinding to stabilize at 3.5, and placing it in refrigerator for later use. Methods Seven-peptide amide (3-9 segment) was synthesized from benzyloxycarboyl leucine p-nitrophenyl ester by 2. chemical synthesis method, then benzyloxycarbonyl-S-benzylcysteine tyrosyl azide (1-2 segment) was synthesized, and oxytocin was synthesized in the third step. |
CAS:
50-56-6
MF:
C43H66N12O12S2
MW:
1007.19
EINECS:
200-048-4
MDL No.:
MFCD00076731
Melting point:
192-194°C
alpha
D22 -26.2° (c = 0.53)
Boiling point:
1533.3±65.0 °C(Predicted)
Density
1.1086 (rough estimate)
refractive index
1.6700 (estimate)
storage temp.
2-8°C
solubility
Very soluble in water. It dissolves in dilute solutions of acetic acid and of ethanol (96 per cent).
form
lyophilized powder
pka
pKa ～6.1(free amino group on Cys) (Occasionally);～10(free phenol on Tyr) (Occasionally)
color
White
Water Solubility
Soluble in water.
Merck
13,7049
BRN
3586108
InChIKey
DSZOEVVLZMNAEH-BXUJZNQYSA-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.
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