Name: Acyclovir (Aciclovir)
Brand: Selleck Chemicals
SKU: S1807
Rating: 5 (20 reviews)

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Control de calidad

Lote: Pureza: 99.93%

99.93

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Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Tiempo de incubación	Descripción de la actividad
BSC-1 cells	Function assay		Antiviral activity of the compound was evaluated against the Herpes simplex virus type-1 in BSC-1 cells, IC50=2.6 μM
P3HR-1 cells	Function assay		Effective concentration for the inhibition of Epstein-Barr virus EBV-DNA synthesis in human lymphoblastoid P3HR-1 cells, EC50=6.75 μM
HFF cells	Function assay		Concentration for HSV-1 plaque reduction (VPR) by 50% in HFF cells, EC50=1.1 μM
HFF cells	Function assay		Inhibitory concentration required to reduce HSV-1 induced cytopathogenic effect (CPE) by 50 % in HFF cells, EC50=2.22 μM
human embryonic lung cells	Function assay		Antiviral activity was measured as effective concentration required to reduce Varicella Zoster virus (OKA)-induced plaque formation in human embryonic lung cells, EC50=1.1 μM
HEL cells	Function assay		Compound was tested for anti-viral activity against HSV-1(G) in HEL cells, EC50=1.3 μM
HEL cell	Function assay		Effective concentration required to inhibit Tyrosine kinase (TK+) Varicella-Zoster virus-induced cytopathicity by 50% in OKA strain HEL cell lines, EC50=4.53 μM
HSV-2 MS Vero cells	Function assay		Inhibition of viral cytopathic effect in infected human foreskin fibroblast cell monolayers of HSV-2 MS Vero cells by 50%, EC50=6.2 μM
HSV-1 E-377 Vero cells	Function assay		Inhibition of plaque formation in monolayers of HSV-1 E-377 Vero cells by 50%, EC50=4.4 μM
HSV-1 KOS Vero cells	Function assay		Inhibition of plaque formation in monolayers of HSV-1 KOS Vero cells by 50%, EC50=2.2 μM
HeLa cell	Function assay		Ability to inhibit cytopathogenicity of herpes simplex type 1 virus (G) in HeLa cell culture, IC50=0.19 μM
HEp-2 cells	Function assay		Minimum inhibitory concentration causing 25% inhibition of cytopathic effect induced by Herpes simplex virus-1 (K979) in HEp-2 cells
HeLa cells	Function assay		Inhibition of HSV-1 DNA synthesis in virus-infected HeLa cells, IC50=1.9 μM
human HFF cells	Function assay		Inhibitory concentration of the drug against the cytopathic effect for E-377 strain of herpes simplex virus-1 (HSV-1) in human HFF cells, EC50=0.04 μM
human HFF cells	Function assay		Inhibitory concentration of the drug against the cytopathic effect for MS strain of herpes simplex virus-2 (HSV-2) in human HFF cells, EC50=0.09 μM
MRC-5 cells	Function assay		Antiviral activity in plaque reduction assay was determined against herpes simplex virus type 2 (HSV-2) in MRC-5 cells, IC50=2.5 μM
human lung fibroblasts (MRC-5)	Function assay		Compound was tested for antiviral activity against Herpes Simplex virus Type-1(18189) in human lung fibroblasts (MRC-5)
Raji cells	Function assay		Inhibitory concentration of the drug against the antigen production against P3HR-1 strain of epstein barr virus-2 (EBV) in Raji cells, EC50=2.9 μM
Vero cells	Function assay		Inhibitory activity against herpes simplex virus type 2 (HSV 2) strain 186 in Vero cells, IC50=1.7 μM
BSC-1 cells	Function assay		Effective concentration required to inhibit herpes simplex virus 1 in BSC-1 cells in ELISA, EC50=1.5 μM
HFF cells	Function assay		Effective concentration required to inhibit varicella zoster virus replication in HFF cells, EC50=1.6 μM
HFF cells	Function assay		Effective concentration required to inhibit herpes simplex virus 1 in HFF cells in cytopathic effect (CPE) assay, EC50=0.9 μM
Daudi cells	Function assay		Inhibition of EBV replication in Daudi cells by viral capsid antigen-ELISA, EC50=0.33 μM
african green monkey Vero cells	Function assay	48 h	Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay, EC50=1.87 μM
WI-38 cell	Function assay		Anti viral activity against VZV(pplla strain) in WI-38 cell monolayers, ID50=4 μM
HEL cells	Function assay	4 days	Antiviral activity against HSV1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathogenicity after 4 days, EC50=0.2 μM
HEL cells	Function assay		Antiviral activity against HSV1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathic effect, EC50=0.14 μM
African green monkey Vero 76 cells	Cytotoxicity assay	48-96 h	Cytotoxicity against African green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by crystal violet staining, CC50=13 μM
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Información química, almacenamiento y estabilidad

Peso molecular	225.2	Fórmula	C₈H₁₁N₅O₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	59277-89-3	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Acycloguanosine, ACV, NSC 645011,BW 248U			Smiles	C1=NC2=C(N1COCCO)N=C(NC2=O)N

Solubilidad

In vitro
Lote:

DMSO : 45 mg/mL (199.82 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	2.500mg/ml (11.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	2.500mg/ml (11.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

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

Targets/IC₅₀/Ki	HSV
In vitro	En un ensayo de reducción de placa en células Vero, se determina la sensibilidad al Acyclovir (Aciclovir) de los aislados del virus del herpes simple. Los valores de IC50 son consistentemente 2-3 veces más bajos en B2 en comparación con la cepa H de células Vero. Las cepas de HSV Tipo 2 son 2-10 veces menos sensibles que las cepas de Tipo 1.
In vivo	Acyclovir (Aciclovir) oral en dosis bajas puede ser eficaz en la prevención de la infección por HSV durante el tratamiento con OKT3 de pacientes seropositivos. La continuación de este compuesto durante dos a cuatro semanas después de la finalización de la terapia con OKT3 puede prevenir la aparición de infecciones tardías.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/3913459/ [2] https://pubmed.ncbi.nlm.nih.gov/3025149/ [3] https://pubmed.ncbi.nlm.nih.gov/2652575/

Información del ensayo clínico

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06228430	Not yet recruiting	Healthy Volunteer	International Bio service	February 12 2024	Phase 1
NCT05589688	Not yet recruiting	Obesity	University Hospital Toulouse	January 2024	Phase 1
NCT06058858	Not yet recruiting	Cytomegalovirus Infections\|Acute Leukemia\|B Cell Lymphoma	Assistance Publique - Hôpitaux de Paris	October 1 2023	--
NCT05468619	Recruiting	Herpes Simplex	National Institute of Allergy and Infectious Diseases (NIAID)	September 23 2022	Phase 1

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Acyclovir (Aciclovir) Antiviral químico

Estructura química

Peso molecular: 225.2