Didanosine

Catalog No.S1702

Didanosine Chemical Structure

Molecular Weight(MW): 236.23

Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.

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In DMSO USD 90 In stock
USD 70 In stock
USD 150 In stock
USD 270 In stock
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Biological Activity

Description Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.
Targets
Reverse transcriptase [1]
490 nM
In vitro

Didanosine induces cytoplasmic lipid droplet accumulations, increases lactate production and decreases activities of COX (complex IV) and SDH (part of complex II) in cultured human muscle cells. [1] Didanosine is converted to its active moiety, dideoxyadenosine-5'-triphosphate (ddATP), which inhibits HIV reverse transcriptase and terminates viral DNA growth in the target cell for HIV. [2] Didanosine induces dose-dependent decreases in neurite number, length of the longest neurite in each neuron, and total neurite length per neuron in dissociated DRG cell cultures with 3 days treatment. Didanosine induces a neurite retraction or neurite loss in a dose-dependent manner in dissociated DRG neurons, suggesting that Didanosine may partially contribute to developing peripheral neuropathy. [3] Didanosine potentiates the mutagenicity of Zidovudine in the thymidine kinase (TK) gene of cultured human TK6 lymphoblastoid cells. Didanosine combined with Zidovudine causes a significant increase in micronucleated PCEs and induces a significant increase in Tk mutants, which is associated with loss of the wild-type Tk+ allele. [4] Didanosine depletes mitochondrial DNA (mtDNA) in cultured hepatocytes, this mtDNA depletion is associated with an increased in vitro production of lactate. [5]

Protocol

Solubility (25°C)

In vitro DMSO 47 mg/mL (198.95 mM)
Water 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 236.23
Formula

C10H12N4O3

CAS No. 69655-05-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00928187 Completed HIV|HIV Infections French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Gilead Sciences|Janssen Pharmaceutica November 2009 Phase 3
NCT00668356 Suspended HIV Infections Assistance Publique - Hôpitaux de Paris September 2009 Phase 2
NCT00091936 Completed HIV Infections|Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) August 2009 --
NCT00427297 Terminated HIV Infections University of Washington|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) September 2007 Phase 3
NCT00364793 Completed HIV Infections Bristol-Myers Squibb February 2007 Phase 1|Phase 2
NCT00332306 Unknown status Tuberculosis|Human Immunodeficiency Virus Infections Tuberculosis Research Centre, India|National AIDS Control Organisation|Indian Council of Medical Research June 2006 Phase 3

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID