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CAS NO.28860-95-9
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C10H14N2O4 |
| Molar Mass | 226.23 |
| Density | 1.2616 (rough estimate) |
| Melting Point | 203-205° (dec); mp 208° |
| Boling Point | 367.84°C (rough estimate) |
| Specific Rotation(α) | D -17.3° (methanol) |
| Flash Point | 273.5°C |
| Solubility | Slightly soluble in water, very slightly soluble in ethanol (96 per cent), practically |
| Vapor Presure | 5.27E-12mmHg at 25°C |
| Appearance | Solid powder |
| Color | White to Off-White |
| pKa | 3.40±0.14(Predicted) |
| Storage Condition | -20°C |
| Stability | Unstable in Solution |
| Refractive Index | 1.5000 (estimate) |
| MDL | MFCD00889211 |
| Physical and Chemical Properties | Crystal. Melting point 203-205 °c (decomposition). |
| Use | For various causes of Parkinson's disease. |
| pharmacological action and mechanism of action | carbidopa is a peripheral dopa decarboxylase inhibitor. It is not easy to penetrate the blood-brain barrier and does not participate in the metabolism of levodopa in the brain, but it can selectively block the decarboxylation of peripheral levodopa into dopamine, minimizing the formation of peripheral dopamine, so that low doses of levodopa pass through the blood-brain barrier more, so that it decarboxylates in the brain to form the effective blood concentration of dopamine, while also reducing peripheral side effects. |
| pharmacokinetics | oral absorption of this product is fast and incomplete, and the absorption amount is 40% ~ 70%. The plasma protein binding rate was 36%. It cannot penetrate the blood-brain barrier, but it can enter the placenta and can be secreted from milk. 50% ~ 60% metabolites and prototype drugs are quickly excreted from urine and a small amount from feces. This product is combined with levodopa at a ratio of 1 :10, which can make the plasma levodopa concentration 5-10 times higher than that of levodopa alone. It is clinically used for tremor paralysis (Parkinson's disease), combined with levodopa. |
| use | as a decarboxylase inhibitor. The combination of levodopa (Sinemet) is currently one of the first choice drugs for the treatment of paralysis, which can reduce the dose of levodopa and reduce toxic side effects. Used for Parkinson's disease caused by various reasons. |
| production method | synthesis route of Strecker method. 1. Preparation of β-Nitro-β-methyl-3-methoxy-4-hydroxystyrene (Ⅱ) Brown-yellow crystals were obtained by reacting vanillin, toluene, nitroethane, glacial acetic acid and n-butylamine. 2. Preparation of α-(3-methoxy-4-hydroxyphenyl) acetone (Ⅲ) and sodium bisulfite adduct. Heat (II) together with toluene to add iron powder and concentrated hydrochloric acid, filter after the reflux reaction, wash the toluene solution with EDTA aqueous solution, dry with anhydrous sodium sulfate, add sodium bisulfite aqueous solution after filtration, stir, crystallize, filter, and dry to obtain (IV). 3. Preparation of α-hydrazinyl-α-methyl-β-(3-methoxy-4-hydroxyphenyl) propionitrile (V) (N), sodium cyanide, water and ether are mixed and stirred, hydrazine hydrate is added, filtered after the reaction is completed, the filter cake is washed with water, and the (V) is obtained by vacuum drying. 4. Preparation of dl-α-hydrazinyl-α-methyl-β-(3, 4-dihydroxyphenyl) propanol (Ⅵ) 45%-48% hydrobromic acid was cooled to below -8 ℃ and hydrogen chloride was passed to saturation. Then hydrazinonitrile was added in batches and stirred at -8 ℃ for 8h. Put it in the refrigerator overnight. Hydrogen chloride is recovered at 95 ℃ for 3 hours, then the reaction solution is evaporated under reduced pressure, ethanol dissolved residue is added, filtered at room temperature, the filtrate is neutralized with diethylamine until pH is 6.4, then placed in a refrigerator overnight, and then processed to obtain (VI) crude product. Refined with water. 5. Add (Ⅵ), L-carbidopa seed and concentrated hydrochloric acid into boiling water to dissolve, add activated carbon to decolorize and filter, cool the filtrate to 60 ℃, and add a part of L-carbidopa seed under stirring. Then it was reduced to 35 ℃ at a constant speed within 1h, kept warm and stirred for 0.5h, filtered, and the filter cake was dried to obtain L-carbidopa. The mother liquor is supplemented (VI) and the splitting operation is repeated. When the temperature is raised to 60 ℃, D-carbidopa seed can be crossed to split the right-handed body. In this cycle, the left-handed body can be split 6-7 times, and the average split yield is 37.3% (the theoretical split yield is 50%)- |
| category | toxic substances |
| toxicity classification | poisoning |
| acute toxicity | abdominal cavity-rat LD50: 2804 mg/kg; Abdominal cavity-mouse LD50: 468 mg/kg |
| flammability hazard characteristics | thermal decomposition discharges toxic nitrogen oxide smoke |
| storage and transportation characteristics | warehouse low temperature ventilation and drying |
| fire extinguishing agent | water, carbon dioxide, foam, dry powder |
CAS:
28860-95-9
MF:
C10H14N2O4
MW:
226.23
EINECS:
657-445-4
MDL No.:
MFCD00069231
Melting point:
203-205° (dec); mp 208°
alpha
D -17.3° (methanol)
Boiling point:
367.84°C (rough estimate)
Density
1.2616 (rough estimate)
refractive index
1.5000 (estimate)
storage temp.
-20°C
solubility
DMSO (Slightly), Methanol (Slightly)
pka
3.40±0.14(Predicted)
form
powder
color
White to Off-White
Stability:
Unstable in Solution
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.