uitsluitend voor onderzoeksdoeleinden
Cat.Nr.: S1807
| Gerelateerde doelwitten | Integrase Bacterial Antibiotics Anti-infection Fungal COVID-19 Parasite Reverse Transcriptase HIV HCV Protease |
|---|---|
| Overige Antiviral Inhibitoren | Moroxydine HCl Aloperine GS-441524 Oleanolic Acid Harringtonine NGI-1 U-18666A LL-37 acetate Aloin B Lanatoside C |
| 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 de cellijn te bekijken | ||||||
| Moleculair gewicht | 225.2 | Formule | C8H11N5O3 |
Opslag (Vanaf de ontvangstdatum) | |
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| CAS-nr. | 59277-89-3 | SDF downloaden | Opslag van stamoplossingen |
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| Synoniemen | Acycloguanosine, ACV, NSC 645011,BW 248U | Smiles | C1=NC2=C(N1COCCO)N=C(NC2=O)N | ||
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In vitro |
DMSO
: 45 mg/mL
(199.82 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)
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 het gedeelte Oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.
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. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
HSV
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|---|---|
| In vitro |
In een plaque-reductie assay in Vero-cellen wordt de Acyclovir (Aciclovir) gevoeligheid van herpes simplex virusisolaten bepaald. IC50-waarden zijn consistent 2-3 keer lager in B2 vergeleken met de H-stam van Vero-cellen. HSV Type 2 stammen zijn 2-10 keer minder gevoelig dan Type 1 stammen. |
| In vivo |
Laaggedoseerde orale acyclovir (aciclovir) kan effectief zijn in de preventie van HSV-infectie tijdens OKT3-behandeling van seropositieve patiënten. Voortzetting van deze verbinding gedurende twee tot vier weken na het einde van de OKT3-therapie kan het optreden van vertraagde infecties voorkomen. |
Referenties |
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(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Rekrutering | 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 |