Cidofovir

別名:HPMPC, GS 0504

Cidofovir suppresses virus replication by selective inhibition of viral DNA synthesis.

Cidofovir化学構造

CAS No. 113852-37-2

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Cidofovir関連製品

DNA/RNA Synthesis阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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 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
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
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
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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生物活性

製品説明 Cidofovir suppresses virus replication by selective inhibition of viral DNA synthesis.
In Vitro
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. [1] 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. [3]

In Vivo
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. [2]. 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. [4] This chemical inhibits growth of the highly aggressive melanoma tumor arising from mouse melanoma B16 cells grafted subcutaneously in C57B16/J mice. [5]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
  • https://pubmed.ncbi.nlm.nih.gov/2854454/
  • https://pubmed.ncbi.nlm.nih.gov/2168690/
  • https://pubmed.ncbi.nlm.nih.gov/1332603/
  • https://pubmed.ncbi.nlm.nih.gov/2069375/
  • https://pubmed.ncbi.nlm.nih.gov/11069450/

化学情報

分子量 279.19 化学式

C8H14N3O6P

CAS No. 113852-37-2 SDF Download Cidofovir SDFをダウンロードする
Smiles C1=CN(C(=O)N=C1N)CC(CO)OCP(=O)(O)O
保管

In vitro
Batch:

Water : 5 mg/mL

DMSO : Insoluble ( 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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