Citicoline sodium

Catalog No.S3619 Synonyms: CDP-choline

For research use only.

Citicoline (CDP-choline) is an essential intermediate in the synthesis of the major phospholipid of the cell membranes, phosphatidylcholine (PtdCho). It increases plasma adrenocorticotropic hormone (ACTH) levels and potentiates serum thyrotrophin (TSH) levels by activating the central cholinergic system.

Citicoline sodium Chemical Structure

CAS No. 33818-15-4

Selleck's Citicoline sodium has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Citicoline (CDP-choline) is an essential intermediate in the synthesis of the major phospholipid of the cell membranes, phosphatidylcholine (PtdCho). It increases plasma adrenocorticotropic hormone (ACTH) levels and potentiates serum thyrotrophin (TSH) levels by activating the central cholinergic system.
In vitro

Citicoline, is an essential component of cell membrane phospholipids. Citicoline (CDP-choline or cytidinediphosphate choline; cytidine 5′-diphosphocholine) is a complex organic molecule composed of ribose, pyrophosphate, cytosine and choline[3]. Citicoline is very water soluble and has a bioavailability of greater than 90%[1]. Citicoline presented no mitogenic and chemotactic effects on hCMEC/D3; however, it significantly increased wound recovery, spheroid sprouting and strongly induced endothelial tube-like structure formation in Matrigel. Citicoline induced the expression of phospho-extracellular-signal regulated kinase (ERK)-1/2. It protects hCMEC/D3 against cell damage/apoptosis. Citicoline induces angiogenesis and improves survival of human brain microvessel endothelial cells through pathways involving p-ERK1/2, and IRS-1[3].

In vivo Citicoline increases nerve cell membrane phospholipids and reduces free fatty acid accumulation. citicoline could reverse the neurologic deficits in a rat model of temporary ischemia with reperfusion[1]. The compound is quickly catabolized, and the products arising are subsequently available for diverse biosynthetic pathways and ultimately excreted as carbon dioxide. The lack of acute and chronic toxicity of citicoline has been repeatedly confirmed in rodents and dogs[2]. citicoline may protect the ischemic neurons by providing a negative effect on the activation of the caspase apoptotic pathway. citicoline has vascular protective, and pro-angiogenic effects[3].

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: human brain microvessel endothelial cells (hCMEC/D3)
  • Concentrations: 10 μM
  • Incubation Time: 4 h
  • Method:

    hCMEC/D3 are cultured in complete medium at a concentration of 5 × 104 cells/ml on collagen pre-coated coverslips for 4 h-incubation. Then, the medium is replaced with serum-free medium and the cells are incubated. After 24 h incubation, the cells are pre-incubated with 10 μM citicoline for 4 h prior to apoptosis induction. After the pre-incubation with citicoline, apoptosis is induced using calcium ionophore (10 μM/24 h); or staurosporin: 10 μM/4 h or by exposure to oxygen-deprivation (12 h, 1% O2).

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Rats
  • Dosages: 50 or 250 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

Water 100 mg/mL
(195.95 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.31
Formula

C14H26N4O11P2.Na

CAS No. 33818-15-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C[N+](C)(C)CCOP(=O)([O-])OP(=O)([O-])OCC1C(C(C(O1)N2C=CC(=NC2=O)N)O)O.[Na+]

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05000190 Not yet recruiting Dietary Supplement: Active capsule|Other: Placebo capsule Attention PepsiCo Global R&D August 30 2021 Not Applicable
NCT05154903 Recruiting Drug: Citicoline 500 MG Acute Ischemic Stroke Ain Shams University|Kafrelsheikh University July 22 2021 Phase 3
NCT04003090 Completed Drug: Citicoline Neurodegenerative Diseases Istituto di Ricerca Neuroftalmologia S.r.l.|Fondazione G.B. Bietti IRCCS March 21 2018 Not Applicable
NCT04422743 Terminated Dietary Supplement: Citicoline 500 mg plus Homotaurine 50 mg Glaucoma IRCCS Policlinico S. Matteo January 25 2018 Not Applicable
NCT02823106 Withdrawn Drug: Verapamil and Citicoline|Other: Placebo Ischemic Stroke Justin Fraser|University of Kentucky August 2016 Phase 1
NCT04009980 Completed Other: OMK2 group|Other: Placebo group Diabetic Retinopathy Fondazione G.B. Bietti IRCCS September 23 2015 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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