Didanosine 69655-05-6

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Molecular Weight:

236.23 Didanosine is a Reverse Transcriptase Inhibitor with an IC50 of 0.49 μM.

Biological Activity

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. 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.


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. 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. Didanosine depletes mitochondrial DNA (mtDNA) in cultured hepatocytes,
this mtDNA depletion is associated with an increased in vitro production
of lactate.

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Product Categories : Microbiology > Reverse Transcriptase Inhibitor