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別名: HPMPC, GS 0504 中文名稱:西多福韋
Cidofovir通過選擇性抑制病毒DNA的合成而抑制病毒復(fù)制。
Cidofovir Chemical Structure
CAS: 113852-37-2
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | 17961851 | |
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 | 17961851 | |
HFF | Proliferation assay | 3 days | Antiproliferative activity against HFF after 3 days by coulter counter assay, EC50=1.9 μM | 19029322 | |
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 | 18852271 | |
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 | 19770274 | |
HEL cells | Function assay | Compound was tested for anti-viral activity against HSV-1(KOS) in HEL cells, EC50=0.57 μM | 14643328 | ||
MRC-5 cells | Function assay | Inhibitory activity against cytopathic effect of HSV-2(E 194) in MRC-5 cells, IC50=10 μM | 8632439 | ||
NHDF cells | Function assay | Inhibitory activity against replication of HCMV in NHDF cells, IC50=0.5 μM | 8632439 | ||
HFF cells | Function assay | Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as reduction in cytopathogenicity, EC50=3.2 μM | 16603351 | ||
HFF cells | Function assay | Antiviral activity against Cowpox virus Brighton in HFF cells assessed as reduction in cytopathogenicity, EC50=7.1 μM | 16603351 | ||
HFF cells | Function assay | Antiviral activity against vaccinia virus Copenhagen measured as cytopathogenicity in HFF cells, EC50=6.9 μM | 16722657 | ||
bone marrow cells | Cytotoxicity assay | Cytotoxicity against human bone marrow cells assessed as inhibition of colony forming unit of granulocyte/macrophage, IC50=10 μM | 16814545 | ||
HFF cells | Function assay | Antiviral activity against Human CMV T2241 in HFF cells by SEAP assay, IC50=0.3 μM | 17043128 | ||
MRC5 cells | Function assay | Antiviral activity against Human CMV Towne in MRC5 cells by PRA, IC50=0.3 μM | 17043128 | ||
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 | 17420214 | ||
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 | 17438061 | ||
HFF cells | Function assay | Antiviral activity against Cytomegalovirus CMV T2211 infected in HFF cells by SEAP reporter gene assay, EC50=0.22 μM | 17709468 | ||
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 | 19226140 | ||
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 | 19226140 | ||
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 | 19226140 | ||
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 | 19226140 | ||
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 | 20585112 | ||
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 | 21376429 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Cidofovir通過選擇性抑制病毒DNA的合成而抑制病毒復(fù)制。 |
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體外研究(In Vitro) | ||||
體外研究活性 | Cidofovir處理培養(yǎng)的細胞,抑制人類巨細胞病毒(HCMV)感染。Cidofovir抑制巨細胞病毒(CMV)蝕斑形成,即使是感染后48小時后加入到細胞中,作用于Davis和AD-169株時IC50分別為0.9 μg/mL和1.6 μg/mL。[1] Cidofovir也抑制單純皰疹病毒感染。此外,Cidofovir作用于猴腎細胞,抑制HSV-1誘導(dǎo)的細胞融合,也抑制HSV-1特異性蛋白的表達和病毒DNA的合成。[3] |
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體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | Cidofovir 每天按5 mg/kg劑量皮下注射給藥受感染的豚鼠,持續(xù)給藥5天,顯著降低血,脾,肺,和唾液腺中病毒傳染力。Cidofovir處理受感染的動物,顯著降低淋巴細胞增多和脾臟的平均組織指數(shù)。[2] Cidofovir作用于皮內(nèi)感染與HSV-1或HSV-2的無毛小鼠,抑制所有臨床表現(xiàn)(皮膚損傷,后腿癱瘓,和死亡)。Cidofovir最顯著的特點是感染后到直至第4天才單獨給藥,也顯著抗HSV-1或HSV-2感染。[4] Cidofovir作用于皮下移植小鼠黑色素瘤B16細胞的C57B16/J小鼠,抑制產(chǎn)生的高度侵襲性的黑色素瘤的生長。[5] |
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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 |
分子量 | 279.19 | 分子式 | C8H14N3O6P |
CAS號 | 113852-37-2 | SDF | Download Cidofovir SDF |
Smiles | C1=CN(C(=O)N=C1N)CC(CO)OCP(=O)(O)O | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
Water : 5 mg/mL (17.9 mM) DMSO : Insoluble ( ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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