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Zidovudine Reverse Transcriptase inhibitor

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.
Zidovudine Reverse Transcriptase inhibitor Chemical Structure

Estructura química

Peso molecular: 267.24

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Control de calidad (Quality Control)

Lote: Pureza: 99.90%
99.90

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 267.24 Fórmula

C10H13N5O4

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 30516-87-1 Descargar SDF Almacenamiento de soluciones madre

Sinónimos Azidothymidine, NSC 602670 Smiles CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-]

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 53 mg/mL (198.32 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 53 mg/mL

Water : 26 mg/mL

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC50/Ki
Reverse transcriptase
In vitro

Zidovudine pretreatment has potent anti-HIV-1 activity in the newly infected T and monocytic cells but not in chronically infected cells. 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. This compound and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. 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. 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. This compound could decrease the HDR efficiency. It decrease CRISPR-mediated sequence-specific genome knockin events while increases knockout efficiency .
Referencias
  • [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/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
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

Preguntas frecuentes (Frequently Asked Questions)

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

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