Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Cidofovir

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Cidofovir DNA/RNA Synthesis inhibitor

Kat.-Nr.: S1516

Cidofovir suppresses virus replication by selective inhibition of viral DNA synthesis.
Cidofovir DNA/RNA Synthesis inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 279.19

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.97%
99.97

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
HEL cells Function assay Compound was tested for anti-viral activity against HSV-1(KOS) in HEL cells, EC50=0.57 μM
MRC-5 cells Function assay Inhibitory activity against cytopathic effect of HSV-2(E 194) in MRC-5 cells, IC50=10 μM
NHDF cells Function assay Inhibitory activity against replication of HCMV in NHDF cells, IC50=0.5 μM
HFF cells Function assay Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as reduction in cytopathogenicity, EC50=3.2 μM
HFF cells Function assay Antiviral activity against Cowpox virus Brighton in HFF cells assessed as reduction in cytopathogenicity, EC50=7.1 μM
HFF cells Function assay Antiviral activity against vaccinia virus Copenhagen measured as cytopathogenicity in HFF cells, EC50=6.9 μM
bone marrow cells Cytotoxicity assay Cytotoxicity against human bone marrow cells assessed as inhibition of colony forming unit of granulocyte/macrophage, IC50=10 μM
HFF cells Function assay Antiviral activity against Human CMV T2241 in HFF cells by SEAP assay, IC50=0.3 μM
MRC5 cells Function assay Antiviral activity against Human CMV Towne in MRC5 cells by PRA, IC50=0.3 μM
UC1B cells Function assay Antiviral activity against Murine polyomavirus MN/RDE Toronto in mouse UC1B cells assessed as reduction of virus-induced cytopathogenicity, EC50=13 μM
african green monkey Vero cells Function assay Antiviral activity against Herpes simplex virus 1 F infected in african green monkey Vero cells assessed as plaque reduction after 36 to 48 hrs, EC50=14.4 μM
HEL cells Function assay 3 days Antiviral activity against HCMV AD169 infected in HEL cells assessed as reduction of virus-induced cytopathogenicity after 3 days, EC50=0.41 μM
HEL cells Function assay 3 days Antiviral activity against HCMV Davis infected in HEL cells assessed as reduction of virus-induced cytopathogenicity after 3 days, EC50=0.41 μM
HFF cells Function assay Antiviral activity against Cytomegalovirus CMV T2211 infected in HFF cells by SEAP reporter gene assay, EC50=0.22 μM
HEL cells Function assay Antiviral activity against ganciclovir-resistant HCMV AD169 clone 4 infected in HEL cells assessed as inhibition of virus-induced cytopathicity, EC50=0.74 μM
HEL cells Function assay Antiviral activity against HCMV Davis infected in human HEL cells assessed inhibition of virus-induced cytopathicity after 7 days postinfection, EC50=0.5 μM
HEL cells Function assay Antiviral activity against HCMV AD169 infected in human HEL cells assessed inhibition of virus-induced cytopathicity after 7 days postinfection, EC50=0.3 μM
HEL cells Function assay Antiviral activity against foscarnet-resistant HCMV AD169 clone C infected in HEL cells assessed as inhibition of virus-induced cytopathicity, IC50=0.045 μM
HFF Proliferation assay 3 days Antiproliferative activity against HFF after 3 days by coulter counter assay, EC50=1.9 μM
HeLaS3 cells Function assay 3-5 days Antiviral activity against Vaccinia virus IHD-J ATCC VR-156 infected in HeLaS3 cells after 3 to 5 days by plaque assay, EC50=18.74 μM
HSB2 cells Function assay 7 days Antiviral activity against Human herpesvirus 6 GS infected in human HSB2 cells assessed as decrease in viral DNA accumulation after 7 days, EC50=2.7 μM
A549 cells Function assay Antiviral activity against Human adenovirus type 11p slobitski infected in A549 cells assessed as inhibition of DNA replication by QPCR assay, EC50=16.5 μM
HFF cells Function assay Antiviral activity against Cowpox virus (Brighton Red) infected in human HFF cells assessed as reduction in viral-induced cytopathic effect by neutral red uptake assay, EC50=6.7 μM
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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 279.19 Formel

C8H14N3O6P

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 113852-37-2 SDF herunterladen Lagerung von Stammlösungen

Synonyme HPMPC, GS 0504 Smiles C1=CN(C(=O)N=C1N)CC(CO)OCP(=O)(O)O

Löslichkeit (Solubility)

In vitro
Charge:

Water : 3 mg/mL

DMSO : Insoluble
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

In vitro

Cidofovir inhibits human cytomegalovirus (HCMV) infection in cultured cells. This compound is inhibitory to CMV plaque formation even when added to the cells at 48 hr post infection with IC50 of 0.9 μg/mL for Davis and 1.6 μg/mL for AD-169 strains,respectively. It also inhibits herpes simplex virus infection. In addition, this chemical blocks cell fusion induced by HSV-1 in monkey kidney cells and blocks the expression of HSV-l-specific proteins and the synthesis of viral DNA.

In vivo

Cidofovir (5 mg/kg/day) subcutaneously for 5 days significantly reduces average virus infectivity titer in blood, spleen, lung and salivary gland in infected guinea pigs. This compound significantly reduces lymphocytosis and average tissue indexe of spleen in infected animals. . It suppresses all manifestations (skin lesions, paralysis of the hind legs, and mortality) of hairless mice infected intracutaneously with HSV-1 or HSV-2. The most remarkable feature of this compound is that a single administration of the compound, even as late as 4 days after infection, conferees significant protection against HSV-1 or HSV-2 infection. This chemical inhibits growth of the highly aggressive melanoma tumor arising from mouse melanoma B16 cells grafted subcutaneously in C57B16/J mice.

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/2069375/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11069450/

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT04542252 Completed
Drug Drug Interaction
SymBio Pharmaceuticals
 November 9 2020 Phase 1
NCT01610765 Withdrawn
Herpes Simplex Virus
University of Alabama at Birmingham
 January 2016 Phase 1|Phase 2
NCT01816646 Completed
Blood And Marrow Transplantation
M.D. Anderson Cancer Center|Gilead Sciences
 September 2013 Phase 1
NCT00780182 Completed
Healthy
Chimerix|National Institutes of Health (NIH)
 October 2008 Phase 1