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Didanosine Reverse Transcriptase inhibitor

Cat.No.S1702

Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.
Didanosine Reverse Transcriptase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 236.23

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 236.23 Formula

C10H12N4O3

Storage (From the date of receipt)
CAS No. 69655-05-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC(OC1CO)N2C=NC3=C2N=CNC3=O

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (198.95 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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] This compound 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] It 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. This chemical induces a neurite retraction or neurite loss in a dose-dependent manner in dissociated DRG neurons, suggesting that it may partially contribute to developing peripheral neuropathy. [3] It potentiates the mutagenicity of Zidovudine in the thymidine kinase (TK) gene of cultured human TK6 lymphoblastoid cells. This compound 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] It depletes mitochondrial DNA (mtDNA) in cultured hepatocytes, this mtDNA depletion is associated with an increased in vitro production of lactate. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/18073553/
  • [5] https://pubmed.ncbi.nlm.nih.gov/14767983/

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