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Cidofovir

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Chemical Structure| 113852-37-2 同义名 : GS 0504;HPMPC;(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine;(S)-HPMPC
CAS号 : 113852-37-2
货号 : A370831
分子式 : C8H14N3O6P
纯度 : 99%
分子量 : 279.187
MDL号 : MFCD00866936
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 3 mg/mL(10.75 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • DNA synthesis
描述 Cidofovir is a synthetic nucleotide analog with potent antiviral activity against a wide range of herpes viruses. In A549 cells, the analysis of 50% inhibitory dose (ID50) of cidofovir dihydrate in different strains and serotypes of adenovirus showed that the mean ID50 values for Ad5 wide-type, Ad5 McEwen, Ad14 and Ad8 are 9.5, 7.3, 5.4, and 4.7 μg/mL, respectively[2]. In MRC-5 cells, the ED50 values of cidofovir dihydrate against Hmc wild type, SC16, BW-S, BW-R, MS wild type are 6.5 ± 2.5, 9.3 ± 1.8, 8.5 ± 1.0, 1.1 ± 0.9, and 9.1 ± 1.8 μM, respectively[3].. A graded decrease in the severity of acute conjunctivitis was observed in rabbits received the treatment of 0.1% cidofovir dihydrate, whereas the concentrations at 0.5% and 1% caused a moderate grade of acute conjunctivitis. A significantly reduction in Ad5 ocular titers was shown in 0.5% and 1% cidofovir dihydrate-treated groups compared to the placebo group. The duration of viral ocular shedding in 0.1%, 0.5%, and 1% cidofovir dihydrate-treated groups were 6, 4, and 4 days, compared to 7-day duration in placebo group. The mean ELISA antibody titer was decreased by 0.5% and 1% cidofovir dihydrate 21 days post the inoculation[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
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
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
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02227641 Patients Undergoing Allogeneic... 展开 >> Stem Cell Transplantation 收起 << Phase 1 Phase 2 Unknown March 2017 Germany ... 展开 >> Medical Center Augsburg Recruiting Augsburg, Germany, 86156 Contact: Christoph Schmid, MD, PhD    0049 821 4002736       Principal Investigator: Christoph Schmid, MD, PhD          Charité University Hospital Berlin Recruiting Berlin, Germany, 13353 Contact: Armin H Gerbitz, MD, PhD    ++49 30 450565256    armin.gerbitz@charite.de    Contact: Lutz Uharek, MD, PhD       lutz.uharek@charite.de    Sub-Investigator: Lutz Uharek, MD, PhD          Principal Investigator: Armin Gerbitz, MD, PhD          Universitiy Hospital Erlangen Recruiting Erlangen, Germany, 91054 Contact: Anita Kremer, MD, PhD    ++49 9131 8543183    anita.kremer@uk-erlangen.de    Contact: Bernd Spriewald, MD, PhD    ++49 9131 8543116    bernd.spriewald@uk-erlangen.de    Sub-Investigator: Katja San Niccolo, MD          University of Mainz Recruiting Mainz, Germany, 55131 Contact: Eva Wagner, MD          Principal Investigator: Eva Wagner, MD          University of Munich LMU Recruiting Munich, Germany, 81377 Contact: Johanna Tischer, MD    0049 89 70954240       Principal Investigator: Johanna Tischer, MD          University of Regensburg Not yet recruiting Regensburg, Germany, 93053 Contact: Ernst Holler, MD, PhD    0049 941 9445570       Principal Investigator: Ernst Holler, MD, PhD 收起 <<
NCT03532035 Adenovirus Phase 2 Not yet recruiting December 20, 2019 -
NCT00078533 Cytomegalovirus Infections Phase 1 Completed - United States, Texas ... 展开 >> Houston Methodist Hospital Houston, Texas, United States, 77030 Texas Children's Hospital Houston, Texas, United States, 77030 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.91mL

3.58mL

1.79mL

35.82mL

7.16mL

3.58mL
参考文献

[1]Li SB, Yang ZH, et al. Activity of(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC) against guinea pig cytomegalovirus infection in cultured cells and in guinea pigs. Antiviral Res. 1990 May;13(5):237-52.

[2]Snoeck R, Sakuma T, et al.(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, a potent and selective inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother. 1988 Dec;32(12):1839-44.

[3]de Oliveira CB, Stevenson D, LaBree L, McDonnell PJ, Trousdale MD. Evaluation of Cidofovir (HPMPC, GS-504) against adenovirus type 5 infection in vitro and in a New Zealand rabbit ocular model. Antiviral Res. 1996 Jul;31(3):165-72. doi: 10.1016/0166-3542(95)00962-0. PMID: 8811201.