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    • Cidofovir

      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

      Cidofovir Chemical Structure

      CAS: 113852-37-2

      規(guī)格 價格 庫存 購買數(shù)量
      25mg 811.35 現(xiàn)貨
      100mg 2198.16 現(xiàn)貨
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      細(xì)胞實驗數(shù)據(jù)示例

      細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息(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

      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。
      體外研究(In Vitro)
      體外研究活性

      Cidofovir處理培養(yǎng)的細(xì)胞,抑制人類巨細(xì)胞病毒(HCMV)感染。Cidofovir抑制巨細(xì)胞病毒(CMV)蝕斑形成,即使是感染后48小時后加入到細(xì)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(xì)胞,抑制HSV-1誘導(dǎo)的細(xì)胞融合,也抑制HSV-1特異性蛋白的表達(dá)和病毒DNA的合成。[3]

      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(xì)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(xì)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]

      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/

      化學(xué)信息&溶解度

      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
      批次:

      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)溶解配方
      批次:

      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

      實驗計算

      摩爾濃度計算器

      質(zhì)量 濃度 體積 分子量

      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)

      mg/kg g μL

      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)

      % DMSO % % Tween 80 % ddH2O
      %DMSO %

      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,: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: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: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(jìn)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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