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Zidovudine Reverse Transcriptase inhibitor

Name: Zidovudine
Brand: Selleck Chemicals
SKU: S2579
Availability: InStock
Rating: 5 (22 reviews)

Cat.No.S2579

Zidovudine (ZDV, Azidothymidine, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. This compound could decrease the HDR efficiency and decrease CRISPR-mediated sequence-specific genome knockin events while increaseing knockout efficiency.

Chemical Structure

Molecular Weight: 267.24

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.90%

99.90

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV CMV Neuraminidase HCV Thioredoxin Reductase HSV RSV Enterovirus 3C-Like Protease Ribosomal Peptidyl Transferase HPV
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
human C8166 cells	Function assay			Antiviral activity against Human immunodeficiency virus 1 infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect, EC50=4e-06 μM
PBMC	Function assay	1 μM		Antiviral activity against HIV1 TEKI replication in PBMC at 1 uM, IC50=0.00014 μM
human H9 cells	Function assay		6 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.3 nM
AA5 cells	Function assay			Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.3 nM
CEM cells	Function assay			Concentration of the drug resulting in 50% reduction of the viral cytopathic effect against HIV-1 replication in CEM cells, EC50=0.32 nM
MT4 cells	Function assay		4 days	Antiviral activity against HIV1 3B assessed as inhibition of virus-induced cytopathogenicity in MT4 cells after 4 days by MTT assay, EC50=0.7 nM
human MT2 cells	Function assay		1 h	Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=1.2 nM
C8166 cells	Function assay			Inhibition of HIV1-3B replication in C8166 cells, EC50=1.9 nM
CEM-SS cell	Function assay			Inhibitory activity against the HIV-1-induced cytopathic effect in CEM-SS cell line, IC50=0.002 μM
PBLs	Function assay			Antiviral activity against subtype isolate G strain in PBLs (peripheral blood lymphocytes), IC50=0.002 μM
human lymphocyte CEM/0 cell line	Function assay			Anti HIV-1 activity in human lymphocyte CEM/0 cell line, EC50=0.003 μM
Jurkat cell	Function assay			Inhibitory concentration against HIV-1 infected Jurkat cell lines, IC50=0.01 μM
human H9 cells	Cytotoxicity assay		6 days	Cytotoxicity against human H9 cells after 6 days by MTT assay, EC50=0.01 μM
C3H/3T3 cells	Function assay			Concentration of compound required to inhibit HIV-1 induced cytopathogenicity of MSV-induced transformation of C3H/3T3 cells by 50%, EC50=0.02 μM
U937 cells	Function assay			Effective concentration required for antiviral activity against Macrophage cell line of U937 cells of Human by XTT assay, EC50=0.03 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	267.24	Formula	C₁₀H₁₃N₅O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	30516-87-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Azidothymidine, NSC 602670			Smiles	CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-]

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (198.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 53 mg/mL

Water : 26 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.650mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 53 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.440mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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]
In vitro	Zidovudine pretreatment has potent anti-HIV-1 activity in the newly infected T and monocytic cells but not in chronically infected cells. ^[1] Inhibition of reverse transcription by this compound decreases p24 antigen levels modestly, decreased HIV-1 gag by 19-fold, and inhibits detection of 2-LTR HIV-1 DNA. ^[2] This compound and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. ^[3] This chemical (AZT, 0.1-50 mM) has a concentration dependent suppressive effect on the growth of granulocyte-monocyte colony forming unit (CFU-GM) derived colonies. This compound exposure also induces a concentration dependent suppressive effect (35-90%) on GM-CSF receptor type alpha (GM-CSFR alpha) gene expression. It causes a much lower decrease (15-22%) on the IL-3 receptor type alpha (IL-3R alpha) message level, and has an insignificant effect on glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and c-myc message levels. ^[4] This chemical causes a concentration-dependent inhibition in the levels of the mRNA of Epo receptors and c-fos, whereas the level of c-myc mRNA is unaffected. It also inhibits protein kinase C (PKC) activity in a concentration- and time-dependent manner, causing 50% inhibition at 10 mM within 3 hours. This compound-induced down-regulation of Epo receptors and c-fos expression coupled with inhibition of Epo receptor-mediated signal transduction through PKC are significant contributory factors to AZT-induced erythroid toxicity. ^[5] This compound could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency^[6] .
References	[1] https://pubmed.ncbi.nlm.nih.gov/9001825/ [2] https://pubmed.ncbi.nlm.nih.gov/10335865/ [3] https://pubmed.ncbi.nlm.nih.gov/8634344/ [4] https://pubmed.ncbi.nlm.nih.gov/12084393/ [5] https://pubmed.ncbi.nlm.nih.gov/7646543/ [6] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4461869/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03991013	Completed	HIV Infections	University of Cape Town\|Wellcome Trust\|Médecins Sans Frontières Belgium	August 8 2019	Phase 2
NCT03642704	Completed	Mother to Child HIV Transmission	ANRS Emerging Infectious Diseases	February 22 2017	Phase 4

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
Do you happen to have any information regarding its half-life?

Answer:
Its half-life in human is available (http://www.rxlist.com/retrovir-drug/clinical-pharmacology.htm), about 0.5-3 hours in adult subjects.

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