Zidovudine

別名:Azidothymidine, NSC 602670

Zidovudine (ZDV, Azidothymidine, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV.

Zidovudine 化学構造

CAS No. 30516-87-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 19200 国内在庫あり
JPY 15900 国内在庫あり
JPY 144600 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(18)

製品安全説明書

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Zidovudine 関連製品

Reverse Transcriptase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
PBMC Function assay 1 μM Antiviral activity against HIV1 TEKI replication in PBMC at 1 uM, IC50=0.00014 μM 16420027
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 20086149
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 17964796
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 18316521
human H9 cells Cytotoxicity assay 6 days Cytotoxicity against human H9 cells after 6 days by MTT assay, EC50=0.01 μM 20846868
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 21534540
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 20086149
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 2153206
C8166 cells Function assay Inhibition of HIV1-3B replication in C8166 cells, EC50=1.9 nM 16279773
CEM-SS cell Function assay Inhibitory activity against the HIV-1-induced cytopathic effect in CEM-SS cell line, IC50=0.002 μM 7650678
PBLs Function assay Antiviral activity against subtype isolate G strain in PBLs (peripheral blood lymphocytes), IC50=0.002 μM 11708913
human lymphocyte CEM/0 cell line Function assay Anti HIV-1 activity in human lymphocyte CEM/0 cell line, EC50=0.003 μM 8478904
Jurkat cell Function assay Inhibitory concentration against HIV-1 infected Jurkat cell lines, IC50=0.01 μM 7837220
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 2016718
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 7932526
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生物活性

製品説明 Zidovudine (ZDV, Azidothymidine, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV.
Targets
Reverse transcriptase [1]
In Vitro
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 Zidovudine decreases p24 antigen levels modestly, decreased HIV-1 gag by 19-fold, and inhibits detection of 2-LTR HIV-1 DNA. [2] Zidovudine and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. [3] Zidovudine (AZT, 0.1-50 mM) has a concentration dependent suppressive effect on the growth of granulocyte-monocyte colony forming unit (CFU-GM) derived colonies. Zidovudine exposure also induces a concentration dependent suppressive effect (35-90%) on GM-CSF receptor type alpha (GM-CSFR alpha) gene expression. Zidovudine 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] Zidovudine 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. Zidovudine also inhibits protein kinase C (PKC) activity in a concentration- and time-dependent manner, causing 50% inhibition at 10 mM within 3 hours. Zidovudine-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] Zidovudine could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency[6] .

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

化学情報

分子量 267.24 化学式

C10H13N5O4

CAS No. 30516-87-1 SDF Download Zidovudine SDFをダウンロードする
Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-]
保管

In vitro
Batch:

DMSO : 53 mg/mL ( (198.32 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 53 mg/mL

Ethanol : 18 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問(FAQ)

質問1:
Do you happen to have any information regarding the half-life of AZT?

回答
The Half-life of S2579 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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