1. Anti-infection
    Cell Cycle/DNA Damage
  2. HIV
    CRISPR/Cas9
  3. Zidovudine

Zidovudine (Synonyms: Azidothymidine; AZT; ZDV)

Cat. No.: HY-17413 Purity: 99.96%
Handling Instructions

Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency.

For research use only. We do not sell to patients.

Zidovudine Chemical Structure

Zidovudine Chemical Structure

CAS No. : 30516-87-1

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10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
100 mg USD 72 In-stock
Estimated Time of Arrival: December 31
500 mg USD 156 In-stock
Estimated Time of Arrival: December 31
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Description

Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency.

IC50 & Target[1][2]

HIV-1

 

CRISPR/Cas9

 

In Vitro

Zidovudine inhibits SVG, Primary human fetal astrocytes (PFA), peripheral blood mononuclear cells (PBMC), and monocyte-derived macrophages (MDM) with EC50 of 17, 1311, 8, and 5 nM, respectively. Zidovudine inhibits SVG, PFA, PBMC, and MDM with EC90 of 0.205 μM, 44.157 μM, 0.481 μM, and 0.219 μM, respectively[1]. Genome editing via CRISPR/Cas9 has become an efficient and reliable way to make precise, targeted changes to the genome of living cells. CXCR4 is a co-receptor for the human immunodeficiency virus type 1 (HIV-1) infection and has been considered as an important therapeutic target for AIDS. CXCR4 mediates viral entry into human CD4+ cells by binding to envelope protein, gp120. Human CXCR4 gene is efficiently disrupted by CRISPR/Cas9-mediated genome editing, leading to HIV-1 resistance of human primary CD4+ T cells. The Cas9-mediated ablation of CXCR4 demonstrated high specificity and negligible off-target effects without affecting cell division and propagation[2].

In Vivo

Intravitrous injection of the NRTIs Lamivudine (3TC), Zidovudine (AZT), or Abacavir (ABC) suppresses the laser-induced choroidal neovascularization (CNV) in wild-type mice compared to PBS vehicle. The mean level of VEGF-A in the RPE/choroid, which peaks on day 3 after laser injury, is significantly reduced in 3TC-, AZT- and ABC-treated eyes compared with control eyes in wild-type mice, but not inP2rx7-/- mice[3].

Clinical Trial
Molecular Weight

267.24

Formula

C₁₀H₁₃N₅O₄

CAS No.

30516-87-1

SMILES

O=C(C(C)=CN1[[email protected]@H](C2)O[[email protected]@H]([[email protected]]2N=[N+]=[N-])CO)NC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (374.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7420 mL 18.7098 mL 37.4195 mL
5 mM 0.7484 mL 3.7420 mL 7.4839 mL
10 mM 0.3742 mL 1.8710 mL 3.7420 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Assays are performed in all cell types in the presence of titrating concentrations of ARV. 5,000 SVG, 2,500 PFA, 200,000 PBMC, or 50,000 MDM cells/well are seeded into triplicate wells of 96-well plates. Twenty-four hours later, the culture medium is removed and replaced with medium containing the ARV or DMSO (0.5% vol/vol), and equivalent TCID50 infectious units of luciferase reporter virus are added to the cells. After a 16 h incubation at 37°C, the initial viral inoculum is removed and replaced with culture medium containing the same antiretroviral drug (ARV) or DMSO (0.5% vol/vol) concentrations. At 72 h post infection, the medium is aspirated, the cells are lysed and HIV-1 infection measured using the Luciferase Assay System. Luminescence is measured using a FLUOStar Optima microplate reader. Inhibition curves and the 50% (EC50) and 90% (EC90) effective concentrations are determined by nonlinear regression analysis, using GraphPad Prism software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
C57BL/6J (wild-type) and P2rx7-/- mice are used. The Nlrp3-/- mice are used. The NRTIs 3TC, AZT, and ABC or the P2X7 antagonist A438079 hydrochloride are dissolved in PBS. For CNV, each group of mice is injected once with 1 μL of NRTIs (3TC, 125 ng/μL; ABC, 183 ng/μL; AZT, 146 ng/μL), 1 μL of A438079 hydrochloride (3, 30, or 300 ng/μL), or the same volume of vehicle (PBS) into the vitreous humor using a 33-gauge needle immediately after laser injury. Another group of mice is injected with 3TC (125 ng) in combination with an anti-mouse VEGF polyclonal antibody (10 ng). Goat whole IgG (10 ng) is used as a biological control for the anti-mouse VEGF antibody.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

ZidovudineAzidothymidineAZTZDVHIVCRISPR/Cas9Human immunodeficiency virusInhibitorinhibitorinhibit

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