| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Citicoline Sodium acts as a PLA2 inhibitor and acetylcholine receptor inducer. It serves as an endogenous intermediate in the synthesis of phosphatidylcholine, providing choline for the biosynthesis of the neurotransmitter acetylcholine. By inhibiting ROS and apoptosis, it exerts neuroprotective effects. The compound also supports brain energy metabolism and enhances memory and focus. Its primary targets are involved in phospholipid metabolism and neurotransmitter synthesis.
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| ln Vitro |
Citicoline Sodium inhibits reactive oxygen species (ROS) and apoptosis in vitro. It promotes neurotransmitter synthesis and brain energy metabolism. The compound has been shown to have protective effects in cerebral ischemia, traumatic brain injury, and memory disorders. It also inhibits PLA2 activity and induces acetylcholine receptor expression. These activities contribute to its neuroprotective and nootropic effects.
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| ln Vivo |
In vivo, Citicoline Sodium has been investigated for the treatment of mania, stroke, hypomania, cocaine abuse, and bipolar disorder. It demonstrates protective effects in cerebral ischemia, traumatic brain injury, and neurodegenerative disorders. The compound supports recovery in ischemic stroke and traumatic brain injury, and improves cerebral blood flow. Its neuroprotective and nootropic effects have been demonstrated in various animal models.
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| Enzyme Assay |
In vitro assays for Citicoline Sodium typically measure its effects on phospholipid synthesis and neurotransmitter metabolism. Cells are treated with citicoline sodium, and the incorporation of choline into phosphatidylcholine is measured using radiolabeled precursors. Acetylcholine levels may be measured by HPLC or enzymatic assays. ROS production is measured using fluorescent probes such as DCFH-DA. Apoptosis is assessed by caspase activity assays or Annexin V staining.
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| Cell Assay |
Cellular assays for Citicoline Sodium are performed using neuronal cell lines (e.g., SH-SY5Y, PC12) or primary neurons. Cells are treated with citicoline sodium at concentrations ranging from 10 to 1000 μM for 24-72 hours. Cell viability is assessed using MTT or LDH release assays. ROS production is measured using fluorescent probes. Apoptosis is assessed by flow cytometry using Annexin V staining or by caspase activity assays.
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| Animal Protocol |
In vivo animal studies with Citicoline Sodium are conducted in rodent models of cerebral ischemia, traumatic brain injury, and neurodegenerative diseases. In the cerebral ischemia model, animals undergo middle cerebral artery occlusion (MCAO) and are treated with citicoline sodium at doses of 100-1000 mg/kg. Neurological deficits and infarct size are assessed. In traumatic brain injury models, cognitive function and histopathology are evaluated.
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| ADME/Pharmacokinetics |
Citicoline Sodium is well absorbed and is metabolized to cytidine and choline, which cross the blood-brain barrier. It is an endogenous compound, and its pharmacokinetics follow normal metabolic pathways. The compound is primarily excreted as carbon dioxide and urine. Its half-life is short, requiring frequent dosing in some studies. For research use, it is typically dissolved in water or saline.
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| Toxicity/Toxicokinetics |
Citicoline Sodium is generally well tolerated with a favorable safety profile. It is an endogenous compound and is not associated with significant toxicity at therapeutic doses. In clinical studies, side effects are mild and include gastrointestinal discomfort and headache. No significant organ toxicity has been reported. The compound has been used extensively in clinical research and is considered safe for human use.
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| References |
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| Additional Infomation |
Citicoline is the choline donor in the biosynthesis of choline phosphate glycerol. It has been investigated for the treatment, supportive care, and diagnosis of conditions such as mania, stroke, hypomania, cocaine abuse, and bipolar disorder. Citicoline is a nutritional supplement and a source of choline and cytidine, possessing potential neuroprotective and nootropic effects. Also known as cytidine-5-bisphosphate choline or CDP-choline, it is hydrolyzed in the intestine to cytidine and choline. After absorption, both cytidine and choline are dispersed and used in various biosynthetic pathways, crossing the blood-brain barrier to resynthesize citicoline in the brain, where it is the rate-limiting product of phosphatidylcholine synthesis. This drug can also increase the levels of acetylcholine (ACh), norepinephrine (NE), and dopamine in the central nervous system (CNS). Furthermore, citicoline participates in the preservation of sphingomyelin and cardiolipin, as well as the restoration of Na+/K+-ATPase activity. Citicoline can also increase glutathione synthesis and glutathione reductase activity, and exert an anti-apoptotic effect. Citicoline is a choline donor in the biosynthesis of choline phosphate glycerols.
Citicoline Sodium is a neuroprotective agent and nutritional supplement used for the treatment of stroke, traumatic brain injury, and neurodegenerative disorders. It is also used to enhance memory and cognitive function. The compound is available as a dietary supplement and has been studied in numerous clinical trials. It is not approved by the FDA as a drug but is widely used as a supplement in many countries. |
| Molecular Formula |
C14H25N4NAO11P2
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|---|---|
| Molecular Weight |
510.3
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| Exact Mass |
510.089
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| CAS # |
33818-15-4
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| Related CAS # |
Citicoline;987-78-0;Citicoline-d9 sodium
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| PubChem CID |
36605
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| Appearance |
White to off-white solid powder
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| Melting Point |
259-268°C (dec.)
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
32
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| Complexity |
813
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[N+](C)(C)CCOP(=O)([O-])OP(=O)([O-])OC[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=CC(=NC2=O)N)O)O.[Na+]
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| InChi Key |
YWAFNFGRBBBSPD-OCMLZEEQSA-M
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| InChi Code |
InChI=1S/C14H26N4O11P2.Na/c1-18(2,3)6-7-26-30(22,23)29-31(24,25)27-8-9-11(19)12(20)13(28-9)17-5-4-10(15)16-14(17)21;/h4-5,9,11-13,19-20H,6-8H2,1-3H3,(H3-,15,16,21,22,23,24,25);/q;+1/p-1/t9-,11-,12-,13-;/m1./s1
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| Chemical Name |
sodium;[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] 2-(trimethylazaniumyl)ethyl phosphate
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| Synonyms |
Citicolinesodium; Citicoline Na; Citicoline Sodium
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~195.96 mM)
DMSO : ~1 mg/mL (~1.96 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (195.96 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9596 mL | 9.7982 mL | 19.5963 mL | |
| 5 mM | 0.3919 mL | 1.9596 mL | 3.9193 mL | |
| 10 mM | 0.1960 mL | 0.9798 mL | 1.9596 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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