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Acyclovir (Aciclovir) Antiviral Chimique

Réf. Catalogue: S1807

Acyclovir (Aciclovir) est un analogue nucléosidique synthétique actif contre les herpèsvirus, et il induit une perturbation du cycle cellulaire et l'apoptose dans les cellules leucémiques Jurkat.
Acyclovir (Aciclovir) Antiviral Chimique Chemical Structure

Structure chimique

Poids moléculaire: 225.2

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.93%
99.93

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires Type d'essai Concentration Temps d'incubation Formulation Description de l'activité PMID
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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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire 225.2 Formule

C8H11N5O3

Stockage (À compter de la date de réception)
N° CAS 59277-89-3 Télécharger le SDF Stockage des solutions mères

Synonymes Acycloguanosine, ACV, NSC 645011,BW 248U Smiles C1=NC2=C(N1COCCO)N=C(NC2=O)N

Solubilité (Solubility)

In vitro
Lot:

DMSO : 45 mg/mL (199.82 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

mg/kg g μL

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Targets/IC50/Ki
HSV
In vitro

In a plaque-reduction assay in Vero cells, the Acyclovir (Aciclovir) sensitivity of herpes simplex virus isolates is determined. IC50 Values are consistently 2-3 fold lower in B2 compared with the H strain of Vero cells. HSV Type 2 strains are 2-10-fold less sensitive than Type 1 strains.

In vivo

low-dose oral acyclovir (aciclovir) may be effective in the prevention of HSV infection during OKT3 treatment of seropositive patients. Continuation of this compound for two to four weeks following the conclusion of OKT3 therapy may prevent occurrence of delayed infections.

Références

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT Recrutement Conditions Promoteur/Collaborateurs Date de début Phases
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