Introduction of zidovudine：
Zidovudine is a synthetic thymidine antiviral drug, and it became the first drug approved for the treatment of acquired immunodeficiency syndrome (AIDS). Zidovudine is a water-soluble molecule, which needs a specific transfer protein to enter the cell, and then it is phosphorylated by the corresponding kinase into a triphosphate-active derivative. Then it can achieve antiviral effect by inhibiting the activity of virus reverse transcriptase (RT), terminating the extension of virus DNA chain and inhibiting virus replication, which can improve the clinical symptoms of HIV-infected people and reduce their mortality.
Zidovudine powder is White to Off-white powder.
Zidovudine is easily soluble in methanol, N, N- dimethylformamide or dimethyl sulfoxide, but soluble in ethanol. The solubility in water (25℃): 25mg/ml. Needle-like crystals are obtained from petroleum ether, which is odorless. Decomposition under light.
Zidovudine is an antiviral product with the chemical formula of C10H13N5O4, which is used to treat patients with AIDS or AIDS-related syndromes and HIV infection.
| Product name | Zidovudine |
| CAS | 30516-87-1 |
| Molecular formula | C10H13N5O5 |
| Molecular weight | 283.24 |
| EINECS Number | 623-849-4 |
| Storage condition | 2-8°C |
| Melting point | 113-115 °C (lit.) |
| Solubility | H2O:50 mg/mL |
| Appearance | White to off-white powder |
| Boiling point | 410.43°C (rough estimate) |
| Density | 1.3382 (rough estimate) |
What is the pharmacological mechanism of Zidovudine?
Zidovudine is a synthetic analog of thymidine, in which the 3'-hydroxyl group (-OH) is replaced by an azide group (-N3). In host cells, Zidovudine is converted into activated zidovudine triphosphate by enzymes. The latter competitively inhibits HIV reverse transcriptase, inhibiting the synthesis, transport, integration of viral DNA into the host cell nucleus and viral replication. In cell culture, Zidovudine powder has a synergistic anti-HIV effect with lamivudine, dideoxyinosine, zalcitabine, various protease inhibitors and non-nucleoside reverse transcriptase inhibitors.
Product Specification
| Item | Specification | Results |
| Appearance | white to off-white powder | Complies |
| Related substance (HPLC) | Total impurity ≤0.5% | 0.20% |
| Max single impurity ≤0.1% | 0.06% | |
| Odor | Characteristic | Complies |
| Assay | 99% | 99.80% |
| Sieve analysis | 100% pass 80 mesh | Complies |
| Loss on Drying | ≤1.0% | 0.12% |
| Residue on Ignition | ≤1.0% | 0.09% |
| Heavy Metal | <10ppm | Complies |
| As | <0.1ppm | 0.05ppm |
| Pb | <0.1ppm | 0.05ppm |
| Cd | <0.1ppm | 0.05ppm |
| Residual Solvents | <100ppm | Complies |
| Conclusion: | Conform with USP Standard | |
What are the functions of Zidovudine?
1. Inhibit virus replication
Zidovudine can effectively inhibit the activity of HIV reverse transcriptase, thus blocking the synthesis of virus genome.
2. Enhance immune function
Zidovudine can increase the level of CD4+T lymphocytes, thus enhancing the antiviral ability of the body.
3. Improve clinical symptoms
Zidovudine can relieve typical symptoms such as fever and fatigue caused by AIDS infection.
4. Delay the progress of the disease
Zidovudine can slow down the development of the disease to a serious stage by stabilizing the pathological state after virus infection.
5. Reduce the mortality rate
Zidovudine can reduce the frequency of organ damage and related complications caused by AIDS and curb the risk of death from the source.
HTML5 atlas of Zidovudine
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IR1 of Zidovudine
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What are the differences between zidovudine and lamivudine?
Both zidovudine and lamivudine belong to nucleoside reverse transcriptase inhibitors, and their pharmacological mechanism is to prevent the synthesis of viral DNA chain by binding with retrovirus reverse transcriptase.
1. Zidovudine: Zidovudine powder is an antiretroviral drug, which can interfere with the replication process of HIV-1 virus. It can block the action of viral RNA polymerase and inhibit the transcription activity of virus. In addition, zidovudine also has immunomodulatory effect, which can enhance the function of CD4+T cells and improve the body's immunity.
2. Lamivudine: Lamivudine is also an antiretroviral drug, mainly used to treat AIDS. It can inhibit the replication of HIV-1 virus and reduce the viral load in the body. At the same time, lamivudine can also protect liver function and reduce the risk of liver injury.
Biological activity of zidovudine：
| Describe | Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), which is widely used to treat HIV infection. Zidovudine enhances editing frequency of CRISPR/Cas9 adjustment. |
| In vitro study | Zidovudine inhibited SVG, primary human fetal astrocytes (PFA), peripheral blood mononuclear cells (PBMC) and monocyte-derived macrophages (MDM), with EC50 of 17,113,18 and 5nM, respectively. Zidovudine inhibited SVG,PFA,PBMC and MDM, and EC90 was 0.205μM,44.157μM,0.481μM and 0.219μM respectively. Genome editing by CRISPR/Cas9 has become an effective and reliable method, which can accurately and pertinently change the genome of living cells. CXCR4 is a common receptor of human immunodeficiency virus type 1 (HIV-1) infection and is considered as an important therapeutic target of AIDS. CXCR4 mediates virus entry into human CD4+cells by binding to envelope protein gp120. Genome editing mediated by CRISPR/Cas9 effectively destroys human CXCR4 gene, resulting in HIV-1 resistance of human CD4+T cells. Cas9-mediated CXCR4 ablation showed high specificity and negligible off-target effect without affecting cell division and proliferation. |
| In vivo study | Compared with PBS vector, intraperitoneal injection of NRTI lamivudine (3TC), zidovudine (AZT) or Abacavir (ABC) inhibited laser-induced choroidal neovascularization (CNV) in wild-type mice. The average level of VEGF-A in RPE/choroid, which reached its peak on the 3rd day after laser injury, decreased significantly in 3TC,AZT and ABC treated eyes compared with the control eyes in wild-type mice, but not in P2rx7-. |
| Cell experiment | In the presence of ARV with titrimetric concentration, the determination was made in all cell types. 5,000 SVG, 2,500 PFA, 200,000 PBMC or 50,000 MDM cells/well were inoculated into triplicate wells of 96-well plates. Twenty-four hours later, the medium was removed and replaced with a medium containing ARV or DMSO (0.5% vol/vol), and the luciferase reporter virus equivalent to TCID50 infection unit was added to the cells. After incubation at 37℃ for 16 hours, the initial virus inoculum was removed and replaced with a medium containing the same concentration of antiretroviral drugs (ARV) or DMSO(0.5％% vol/vol). 72 hours after infection, the culture medium was sucked out, cells were lysed and HIV-1 infection was measured by luciferase assay system. Luminescence was measured by FLUOStar Optima enzyme label instrument. The inhibition curve and effective concentrations of 50% (EC50) and 90% (EC90) were determined by nonlinear regression analysis using GraphPad Prism software. |
| Animal experiment | Mice [3] C57BL/6J (wild type) and P2rx7-/-mice were used. Use Nlrp3-/-mice. Dissolve NRTI 3TC, AZT and ABC or P2X7 antagonist A438079 hydrochloride in PBS. For CNV, 1μLNRTIs(3TC, 125 ng /μL; ABC,183 ng /μL; AZT, 146 ng /μL), 1μLA438079 hydrochloride (3,30 or 300) Immediately after laser injury, the same volume of carrier (PBS) was added to vitreous humor (ng /μL) with No.33 needle. Another group of mice were injected with 3TC(125ng) in combination with anti-mouse VEGF polyclonal antibody (10ng). Goat IgG(10ng) was used as the biological control of anti-mouse VEGF antibody. |
| References |
[1]. Gray LR, et al. The NRTIs lamivudine, stavudine and zidovudine have reduced HIV-1 inhibitory activity in astrocytes. PLoS One. 2013 Apr 16;8(4):e62196. [2]. Hou P, et al. Genome editing of CXCR4 by CRISPR/cas9 confers cells resistant to HIV-1 infection. Sci Rep. 2015 Oct 20;5:15577. [3]. Mizutani T, et al. Nucleoside Reverse Transcriptase Inhibitors Suppress Laser-Induced Choroidal Neovascularization in Mice. Invest Ophthalmol Vis Sci. 2015 Nov;56(12):7122-9. |
Side effects of AIDS blockers
At present, there are many kinds of drugs blocking AIDS, including six categories and more than 30 kinds of drugs, most of which have certain side effects, as follows:
1. Lamivudine is relatively safe and has no obvious toxic and side effects;
2. When tenofovir is used for a long time, patients are prone to abnormal calcium and phosphorus metabolism and calcium loss. In addition, there are nephrotoxic reactions, and long-term loss of calcium can cause osteoporosis;
3, efavirenz is prone to nervous system manifestations, such as insomnia, dreaminess, hallucinations, etc., and rash and abnormal liver function can also occur after long-term use;
4. Nevirapine and zidovudine have side effects of bone marrow suppression, including leukopenia and thrombocytopenia, anemia and gastrointestinal irritation.
What are the precautions for using Zidovudine powder?
1. Patients should be reminded of the adverse reactions of other drugs used at the same time.
2. Patients should be warned that the drug has not been proved to prevent the spread of HIV through sexual contact or blood pollution.
3. Zidovudine powder can't cure HIV infection, and patients are still at risk of diseases related to immunosuppression, such as infections caused by conditional pathogens and malignant tumors.
How and where to buy Zidovudine Powder wholesale?
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
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