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CAS NO.64-86-8
98%(1-25)Kilogram98%(26-500)Kilogram98%(501-1000)Kilogram
F
Colchicine
CAS: 64-86-8
Molecular Formula: C22H25NO6
| Molecular Formula | C22H25NO6 |
| Molar Mass | 399.44 |
| Density | 1.2770 (rough estimate) |
| Melting Point | 150-160°C (dec.)(lit.) |
| Boling Point | 522.37°C (rough estimate) |
| Specific Rotation(α) | -250 º (c=1, alcohol) |
| Flash Point | 392.9°C |
| Water Solubility | 45 g/L (20 ºC) |
| Solubility | Soluble in ethanol, chloroform |
| Vapor Presure | 6.21E-21mmHg at 25°C |
| Appearance | White powder |
| Color | white to yellow with a green cast |
| Merck | 14,2471 |
| BRN | 2228813 |
| pKa | 12.36(at 20℃) |
| Storage Condition | 2-8°C |
| Stability | Stable. Light sensitive. Incompatible with strong oxidizing agents. |
| Sensitive | Light Sensitive |
| Refractive Index | 1.5614 (estimate) |
| MDL | MFCD00078484 |
| Physical and Chemical Properties | Light yellow crystal or crystalline powder, taste, taste bitter, see light discoloration. Mp157 ℃ (ethyl acetate recrystallization), specific rotation [α]17D-429 °(1.72%, water), -121 °(0.9%, chloroform), the maximum absorption wavelength in ethanol was 243nm and 350.5nm. This product is soluble in water, ethanol and chloroform, soluble in benzene and ether, insoluble in petroleum ether, 0.5% of this solution is weakly acidic. LD50 (mouse, abdominal cavity) 6.1 mg/kg. |
| Use | Anti-gout and anti-tumor drugs for the treatment of acute gout and cancer |
| alkaloid | colchicine, also known as colchicine, is an alkaloid extracted from the bulbs and seeds of the Liliaceae plant colchicine, it is found naturally in the Liliaceae plant jialanensis (0.11%) and Lijiang (0.1%). Light yellow needle-like crystals. It is slightly odorous and bitter. Melting point 157 ℃, soluble in cold water, alcohol, chloroform and formaldehyde, poor solubility in hot water, not soluble in benzene and ether, almost insoluble in petroleum ether, 0.5% solution pH 5.9, after hydrolysis by ammonia, the toxicity can be reduced. Colchicine has anti-mitotic and anti-tumor effects. In 1889, the effect of colchicine on mitosis was first discovered by an Italian scholar, Pernica, who described that the mitotic phase of the cells in the inner wall of the Dog stomach was suppressed by colchicine and the spindle was destroyed, paralysis of chromosome action, abnormal mitotic cells remain in a large number of metaphase. This abnormal division caused by colchicine is called colchicine mitosis (C-mitosis for short). Colchicine is one of the most widely used chemical agents in karyotype analysis and polyploid mutagenesis. The concentration of the aqueous solution is positively correlated with the efficacy of its action, and the higher the concentration, the stronger the effect. Various plants and different tissues respond differently to colchicine. In summary, the treatment time for young and rapidly dividing tissues (such as the embryo of germinating seeds) can be shorter and the concentration should be lower; Whereas the treatment time can be longer and the concentration should be higher. The effective concentration of colchicine treatment was 0.01~10 ~ 0.4%, and about 0.2% of the most widely used. For example, the concentration of 0.2 ~ 0.4% colchicine solution drops on the growth point of diploid watermelon seedlings, once a day, for 4 consecutive days, and shade to maintain humidity, can induce tetraploid watermelon. For cereal crops, such as rice, the robust seedlings with more than four true leaves can be cut at the root neck, and immersed in 0.025 ~ 0.05% colchicine solution without cutting the growing point, submerged incision, after 8 to 14 days (20 degrees C) can also be obtained tetraploid plants. At present, colchicine is widely used for chromosome doubling of haploid plants obtained from anther (powder) and ovary culture. |
| anti-gout drugs | colchicine has a good effect on acute gout, which can relieve pain quickly and prevent the onset of arthritis, its mechanism of action is related to inhibiting the proliferation and activity of leukocytes and affecting the release of lysosomes. The pharmacological effect of this product is to reduce the activity and phagocytosis of leukocytes in inflammatory tissues, reduce the inflammation caused by uric acid crystals, and thus play an anti-inflammatory, detumescence and analgesic effect, therefore, it has a selective anti-inflammatory effect on acute gouty arthritis. In addition, this product is also a kind of mitotic toxin, which has a strong effect of inhibiting cell division, so that the cell stops in the division phase, resulting in the death of tumor cells, so it can be used for cancer treatment. This product is easy to absorb after oral administration, 30% is combined with plasma protein, the peak time of blood drug concentration is 0.5~2 hours after oral administration, and the peak concentration of 2mg is about 2.2ng/ml, after 12 hours of acute gout administration, the drug effect can be sustained for 50 to 70 hours, and the drug concentration in the isolated neutrophils is higher than the plasma concentration and can be maintained for 10 days. Most of this product is metabolized by the liver, metabolites and prototype drugs are excreted by the bile, reabsorbed by the intestine, not absorbed by the intestine. The remaining about 10% ~ 20% by the kidney with urinary excretion. This product does not affect the formation, dissolution and excretion of uric acid salt, and thus has no effect of lowering blood uric acid. It is clinically used to treat acute attack of gouty arthritis, prevent acute attack of recurrent gouty arthritis, familial Mediterranean fever, leukemia, skin cancer, Hodgkin's disease, aplastic anemia, etc. Also used for breast cancer, lung cancer, esophageal cancer, cervical cancer, nasopharyngeal carcinoma, Hodgkin's disease, chronic myelogenous leukemia, skin cancer and other malignant diseases M stage cycle specific treatment. |
| adverse reactions | and dose size were significantly correlated. 1. Gastrointestinal reactions: Nausea, Abdominal Pain, Diarrhea, Vomit and loss of appetite for the common early adverse reactions, the incidence rate of up to 80%, severe cases can cause dehydration and electrolyte disorders and other performance, such as the reaction immediately discontinued. Long-term users may develop severe hemorrhagic gastroenteritis or malabsorption syndrome. 2. Blood system reaction: Long-term medication can cause agranulocytosis, thrombocytopenia, aplastic anemia, and sometimes life-threatening. 3. Other toxic reactions; Mainly for urethral irritation symptoms, such as frequency, urgency, dysuria, hematuria, Oliguria, and even renal failure. Stomach, pharynx or skin burning sensation, and Fever, bloody Diarrhea, mental changes, myasthenia gravis, respiratory depression and other symptoms. 4. Check hemogram, liver and kidney function during taking colchicine. Hematopoietic insufficiency, liver and kidney damage, severe heart disease and gastrointestinal disease patients should be used with caution. Contraindicated in pregnant women. 5. Muscle, peripheral neuropathy: proximal muscle weakness, and serum creatine kinase increased; Muscle damage in the peripheral nerve axonal polyneuropathy may occur at the same time, manifested as numbness, tingling and weakness; muscle neuropathy is rare, often in the prevention of gout and long-term users and mild renal insufficiency appear. |
| dosage and usage | tablet: 0.5mg per tablet; Injection: 1mg, 2mg. 1. For the treatment of acute gout: adult oral tablets, the first dose of 0.5~1mg, after every 1~2 hours to take 0.5~0.6mg, until the joint symptoms or gastrointestinal symptoms, that is, withdrawal. The general total dose of 4~10mg effective. Note that the earlier the drug is used in the acute phase, the better the effect is. If intravenous injection, the first dose of 1~2mg, with normal saline 20ml slow injection, time of not less than 5 minutes, if necessary, every 6~12 hours intravenous injection of 0.5~1mg, until effective, the total dose of 4~5mg/d. The effect of intravenous injection was better than that of oral administration, and the gastrointestinal reaction was significantly reduced. 2. For the prevention of acute gout: adult tablets 0.5~0.6mg each time, 2 times a day or intravenous injection of 1~2mg/d. 3. For the experimental diagnosis of gout: such as acute joint symptoms after medication relief, that is helpful to confirm the diagnosis. |
Mol Download Chemical properties
CAS:
64-86-8
MF:
C22H25NO6
MW:
399.44
EINECS:
200-598-5
MDL No.:
MFCD00078484
Melting point:
150-160 °C (dec.)(lit.)
alpha
-250 º (c=1, alcohol)
Boiling point:
522.37°C (rough estimate)
Density
1.2770 (rough estimate)
refractive index
1.5614 (estimate)
storage temp.
2-8°C
solubility
H2O: 10 mg/mL
pka
12.36(at 20℃)
form
powder
color
white to yellow with a green cast
Water Solubility
45 g/L (20 ºC)
Sensitive
Light Sensitive
Merck
14,2471
BRN
2228813
BCS Class
3
Stability:
Stable. Light sensitive. Incompatible with strong oxidizing agents.
InChIKey
IAKHMKGGTNLKSZ-INIZCTEOSA-N
LogP
1.300
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.