solo para uso en investigación

Ribavirin (ICN-1229) Antiviral chemical

Cat. No.: S2504

Ribavirin (NSC-163039, ICN-1229, RTCA, Tribavirin), a synthetic guanosine analogue, possesses a broad spectrum of activity against DNA and RNA viruses.
Ribavirin (ICN-1229) Antiviral chemical Chemical Structure

Estructura química

Peso molecular: 244.20864

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.97%
99.97

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
E6SM cell lines Function assay Effective concentration required to inhibit Herpes simplex virus-1(HSV-1) / thymine kinase deficient (TK-)B2006 / VMW1837 induced cytopathicity by 50% in E6SM cell lines, EC50=0.005 μM
MDCK cells Function assay 3 days Antiviral activity against Influenza B virus (B/HK/5/72) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by microscopic analysis, EC50=0.094 μM
mouse L1210 cells Function assay 20-60 mins Inhibition of IMPDH in mouse L1210 cells assessed as formation of [2,8-3H]hypoxanthine from [2,8-3H]IMP after 20 to 60 mins, IC50=1 μM
human CEM cells Function assay 20-60 mins Inhibition of IMPDH in human CEM cells assessed as formation of [2,8-3H]hypoxanthine from [2,8-3H]IMP after 20 to 60 mins, IC50=1 μM
BHK21 cell line Function assay Inhibition of West Nile virus VLP replicon in BHK21 cell line, EC50=1.1 μM
HeLa cell Function assay Effective concentration required to inhibit respiratory synaptial(RSV) virus-induced cytopathicity by 50% in HeLa cell lines, EC50=1.5 μM
MDCK cells Function assay 36 h Antiinfluenza activity against influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 36 hrs, IC50=1.9 μM
MDBK cells Function assay 2 days Antiviral activity against Bovine viral diarrhea virus 1-NADL ATCC VR534 infected in MDBK cells assessed as reduction of viral cytopathic effect after 2 days bt MTS assay, EC50=4.6 μM
african green monkey Vero cells Function assay 5 days Antiviral activity against RSV A2 infected in african green monkey Vero cells after 5 days by plaque reduction assay, EC50=7 μM
HEL cells Function assay 2-3 days Antiviral activity against Herpes simplex virus 1 KOS infected in HEL cells assessed as protection from virus-induced cytopathogenicity after 2 to 3 days by MTT assay, EC50=10 μM
HEK293 cells Function assay 24 h Inhibition of influenza A virus RNA-dependent RNA polymerase expressed in HEK293 cells after 24 hrs by dual luciferase reporter gene assay, EC50=15 μM
human BE(2)-C cells Function assay 18-20 h Antiviral activity against Western equine encephalomyelitis virus infected in human BE(2)-C cells assessed as inhibition of viral RNA replication after 18 to 20 hrs by luciferase reporter gene assay, IC50=16 μM
human HuH7-J20 cells Function assay Antiviral activity against HCV JFH1 infected in human HuH7-J20 cells assessed as inhibition of viral life cycle by measuring secreted alkaline phosphatase level preincubated with cells for 1 hr followed by viral inoculation for 3 hrs measured at 72 hrs, EC50=30.4 μM
human MT4 cells Cytotoxic assay 96 h Cytotoxicity against human MT4 cells after 96 hrs by MTT assay, CC50=31 μM
human HuH7 cells Cytotoxic assay 3 days Cytotoxicity against human HuH7 cells infected with HCV1b after 3 days by MTS assay, CC50=32 μM
human KB cells Function assay 72 h Antiviral activity against Rhinovirus type 13 infected in human KB cells assessed as inhibition of virus-induced cytopathic effect after 72 hrs relative to control
human KB cells Function assay 1-1000 μg/ml 72 h Antiviral activity against Rhinovirus type 13 infected in human KB cells assessed as inhibition of virus-induced cytopathic effect at 1 to 1000 ug/ml after 72 hrs
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 244.20864 Fórmula

C8H12N4O5

Almacenamiento (Desde la fecha de recepción)
Nº CAS 36791-04-5 Descargar SDF Almacenamiento de soluciones madre

Sinónimos NSC-163039, RTCA, Tribavirin Smiles C1=NC(=NN1C2C(C(C(O2)CO)O)O)C(=O)N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 49 mg/mL (200.64 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 49 mg/mL

Ethanol : Insoluble

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)

In vitro
Ribavirin (ICN-1229) significantly reduces the efficiency with which progeny subgenomic replicons transfect new cells in the replicon system, although it has little effect on levels of HCV replication. This compound increases the mutation frequency of HCV, with the highest rates of mutations being found in the NS5A-encoding region. It enhances TH1 while inhibiting T 2 cytokine production by stimulated T cells. Ribavirin shows antiviral activity against a variety of RNA viruses and is used in combination with interferon-alpha to treat hepatitis C virus infection. It reduces infectious poliovirus production to as little as 0. 00001% in cell culture. Its antiviral activity is exerted directly through lethal mutagenesis of the viral genetic material. This compound markedly reduces viral-induced parameters of macrophage activation at physiologic concentrations (up to 500 mg/mL). It inhibits the production of IL-4 by Th2 cells, whereas it does not diminish the production of IFN-gamma in Th1 cells. Ribavirin exhibits antiviral activity against a broad range of both DNA and RNA viruses in vitro. It is a cytostatic agent and causes a reduction in synthesis of DNA, RNA and proteins in exposed cells. It is thought to induce a switch in T-helper cell phenotype from type 2 to type 1.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/9531310/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16287208/

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes PMID
Western blot p53 / p-p53 / p21 / Mdm2 EZH2 / p-ERK / ERK / p-eIF4E / eIF4E / p21 Cyclin D1 p-AKT / AKT / pBP1 / BP1
S2504-WB1
22962590
Growth inhibition assay Cell number
S2504-viability1
21415224

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
NCT05940545 Recruiting
CCHF
Liverpool School of Tropical Medicine
July 12 2023 Phase 1|Phase 2
NCT04283513 Not yet recruiting
Hemorrhagic Fever
U.S. Army Medical Research and Development Command
October 31 2022 Phase 2
NCT04335123 Completed
COVID-19
University of Kansas Medical Center
April 4 2020 Phase 1
NCT04285034 Completed
Lassa Fever
University of Oxford
November 26 2019 --
NCT03889106 Terminated
Lassa Fever
University of Oxford|National Institute for Health Research United Kingdom|Kenema Government Hospital|London School of Hygiene and Tropical Medicine|Public Health England
March 1 2019 --
NCT03585725 Terminated
Follicular Lymphoma|Mantle Cell Lymphoma
Weill Medical College of Cornell University|Memorial Sloan Kettering Cancer Center
September 26 2018 Early Phase 1