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987-78-0

citicoline

CAS: 987-78-0

Molecular Formula: C14H26N4O11P2

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987-78-0 - Names and Identifiers

Name citicoline
Synonyms Haocolin
Neucolis
Hornbest
Citicolina
Difosfocin
NSC 122002
citicoline
Emicholine F
CYTIDINE 5'-DIPHOSPH
Cytidine Diphosphate Choline
CYTIDINE 5'-DIPHOSPHOCHOLINE
5'-O-[hydroxy({[2-(trimethylammonio)ethoxy]phosphinato}oxy)phosphoryl]cytidine
Cytidine 5'-(trihydrogen diphosphate), P'-[2-(trimethylammonio)ethyl] ester, inner salt
CAS 987-78-0
EINECS 213-580-7
InChI InChI=1/C12H22N4O11P2/c1-16(2,3)26-29(22,23)27-28(20,21)24-6-7-9(17)10(18)11(25-7)15-5-4-8(13)14-12(15)19/h4-5,7,9-11,17-18H,6H2,1-3H3,(H3-,13,14,19,20,21,22,23)/t7-,9-,10-,11-/m1/s1

987-78-0 - Physico-chemical Properties

Molecular FormulaC14H26N4O11P2
Molar Mass488.33
Melting Point>185°C (dec.)
Specific Rotation(α)D25 +19.0° (c = 0.86 in H2O)
Solubility Water (Sparingly)
AppearanceSolid
ColorWhite
pKa4.4(at 25℃)
Storage ConditionKeep in dark place,Inert atmosphere,Store in freezer, under -20°C
StabilityMoisture Sensitive
Physical and Chemical PropertiesThe sodium salt of this product is white or white-like powder, odorless; easy to absorb moisture. This product is soluble in water and insoluble in ethanol, acetone and chloroform. It's optically active.
UseFor the treatment of acute craniocerebral trauma and brain surgery, such as disturbance of consciousness

987-78-0 - Risk and Safety

ToxicityLD50 in mice, rats (mg/kg): 4600 ±335, 4150 ±370 i.v.; both species 8 g/kg orally (Grau)

987-78-0 - Nature

Open Data Verified Data
  • This product is white or off-white powder, odorless, with hygroscopicity. This product is soluble in water, ethanol, acetone, chloroform insoluble.
  • It is a precursor for the biosynthesis of lecithin. The molecule contains cholophos and cytosine, which are involved in the transfer of choline to diglycerides during lecithin synthesis. The synthesis of lecithin is increased, which can change the physiological function of meninges. It can also improve cerebral vascular tension, increase cerebral blood flow and oxygen consumption, and has a wake-up effect.
Last Update：2024-01-02 23:10:35

987-78-0 - Use

Open Data Verified Data

It is used for the disturbance of consciousness after acute craniocerebral trauma and cerebral surgery. Cerebral thrombosis, multiple cerebral embolism, paralysis, stroke sequelae, cerebral arteriosclerosis caused by cerebral insufficiency, hypnotic drugs and carbon monoxide poisoning and a variety of organic encephalopathy.

Last Update：2022-01-01 11:12:59

987-78-0 - Safety

Open Data Verified Data

light shielding, closed storage.

Last Update：2022-01-01 11:12:59

987-78-0 - Reference Information

Introduction citicoline, named citicoline in Chinese Pharmacopoeia (2005 edition), chemical name choline cytidine 5 '-diphosphate monosodium salt, it is a precursor of lecithin biosynthesis, and when brain function is reduced, the lecithin content in brain tissue is significantly reduced.
function and mechanism of action citicoline can stabilize cell membrane by stimulating S-adenosyl-L-methionine, the dendritic complexity and spinous process density of motor neuron structure are increased, the plasticity of nerves in non-damaged areas is improved, and the functional recovery is promoted, reducing the level of water-soluble phospholecithin, as well as inhibiting the activity of secretory phospholipase A2(PLA2) or by inhibiting TNF-a/IL-1b, inhibiting PLA2 activation, reducing the loss of phospholipids, so as to increase the synthesis of phosphatidylcholine phosphate, repair nerve cell membrane; Can also increase the expression of anti-apoptotic factors such as Bcl-2 and inhibit the release of glutamic acid to reduce cytotoxicity; it can promote the rapid repair of damaged cell surface and mitochondrial membrane, maintain cell tightness and biological function, and reduce the release of free fatty acids, thereby reducing the production of toxic oxygenated metabolites and free radicals; increases vasopressin and plasma levels of proadrenalin, stimulates the release of growth hormone, thyrotropin and luteinizing hormone.
Application is mainly used for metabolic disorders, disturbance of consciousness, paralysis, nerve deafness and tinnitus after craniocerebral trauma and brain surgery, and hypnotic drug poisoning. Another Parkinson's syndrome, cerebral thrombosis half body paralysis also has good curative effect.
Clinical application citicoline is a single nucleotide composed of nucleic acid, cytosine, Pyrophosphate and choline, in clinic, it is mainly used to treat a variety of neurodegenerative diseases, such as Alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis and so on. Studies have also shown that citicoline can increase the brain's uptake of dopamine and glutamate, thereby improving cognitive performance. Citicoline can also reduce the release of free fatty acids and restore the activity of mitochondrial ATPase and cell membrane Na /K ATPase, thus alleviating brain damage. However, the pathophysiological mechanisms of neurodegenerative diseases are very complex, involving Cholinergic deficiency, glutamate excitotoxicity, neuroinflammation, immune disorders, glucose metabolism decline and blood-brain barrier disruption.
preparation method There are many preparation methods of citicoline sodium, mainly in three ways. One is microbial fermentation. This method has the problems of low product concentration and unstable yield. One is organic chemical synthesis. The method is difficult to separate the product from the condensation agent, is not suitable for medicinal, low reaction conversion rate, more by-products, high cost, serious environmental pollution and so on. There is also an enzymatic synthesis method, such as the use of beer yeast mud and other microorganisms for biosynthesis. Free yeast mud cells were used for enzymatic synthesis with simple process, high conversion rate and low cost. The production process of citicoline sodium by enzymatic synthesis can be divided into two parts: enzymatic synthesis process and extraction and purification process.
Use for disturbance of consciousness after acute craniocerebral trauma and brain surgery. Cerebral thrombosis, multiple cerebral embolism, paralysis, stroke sequelae, cerebral arteriosclerosis caused by cerebral insufficiency, hypnotic drugs and carbon monoxide poisoning and a variety of organic encephalopathy.
This product is a precursor of lecithin biosynthesis, which can promote lecithin biosynthesis. The product can promote the recovery of brain function and awakening. It is suitable for the disturbance of consciousness such as traumatic brain injury and stroke sequelae, and also for the disturbance of consciousness caused by acute injury of central nervous system.
for the treatment of acute craniocerebral trauma and post-operative disturbance of consciousness, etc.
production method can be extracted from liver or yeast, or can be chemically synthesized. In the synthesis method, cytosine -5 '-diphosphate is reacted with ethylenimine to form cytosine -5'-diphosphate aminoethyl Ester, and then methylated with methyl iodide. Cytosine -5 '-phosphate amide can also be obtained by direct condensation with Choline phosphate.
Last Update：2024-04-09 21:11:58
987-78-0
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Nantong Reform Petro-Chemical CO., LTD.
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Suzhou Myland Pharm & Nutrition Inc.
Product Name: Citicoline(CDPC) Request for quotation
CAS: 987-78-0
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Nantong Reform Petro-Chemical CO., LTD.
Spot supply
Product Name: citicoline Request for quotation
CAS: 987-78-0
Tel: +86-17551318830
Email: r@reformchem.com­
Mobile: +86-17551318830
QQ: 3785839865 Click to send a QQ messageSend QQ message
Jiangsu Pules Biotechnology Co.,Ltd.
Product Name: citicoline Request for quotation
CAS: 987-78-0
Tel: 17505222756
Email: pules.cn@gmail.com
Mobile: +86-17551318830
Wechat: 17505222756
Hefei TNJ Chemical Industry Co.,Ltd.
Product Name: citicoline Request for quotation
CAS: 987-78-0
Tel: 0086-551-65418684
Email: sales@tnjchem.com
　　　　 info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840 Click to send a QQ message
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: Cytidine 5-Diphosphocholine Visit Supplier Webpage Request for quotation
CAS: 987-78-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Wechat: 18301782025
Suzhou Myland Pharm & Nutrition Inc.
Product Name: Citicoline(CDPC) Request for quotation
CAS: 987-78-0
Tel: 051266706057
Email: maggie@mylandpharm.com
Mobile: 18656033903
QQ: 1677088563 Click to send a QQ messageSend QQ message
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987-78-0
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