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Acyclovir (Aciclovir) Antiviral Chemische stof

Cat.nr.: S1807

Acyclovir (Aciclovir) is een synthetisch nucleoside-analoog dat actief is tegen herpesvirussen, en het induceert celcyclusverstoring en apoptosis in Jurkat-leukemiecellen.
Acyclovir (Aciclovir) Antiviral Chemische stof Chemical Structure

Chemische structuur

Molecuulgewicht: 225.2

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.93%
99.93

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving 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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 225.2 Formule

C8H11N5O3

Opslag (vanaf de datum van ontvangst)
CAS-nr. 59277-89-3 SDF downloaden Opslag van stamoplossingen

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

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 45 mg/mL (199.82 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (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.

Referenties

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer Werving Aandoeningen Sponsor/medewerkers Startdatum Fasen
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