Cidofovir (GS 0504) 是一种无环单磷酸核苷酸类似物，CMV抑制剂，具有抗病毒活性。Cidofovir 可通过选择性抑制病毒 DNA 聚合酶 (DNA polymerase) 来抑制巨细胞病毒 (CMV) 复制。Cidofovir 可诱导细胞凋亡 (apoptosis)，用于巨细胞病毒性视网膜炎、疱疹、癌症研究。Cidofovir 还具有抗正痘病毒 (orthopoxvirus) 和抗天花病毒活性。
| 生物活性 | Cidofovir (GS 0504) is an acyclic monophosphate nucleotide analogue andCMVinhibitor with antiviral activity. Cidofovir inhibits cytomegalovirus (CMV) replication by selectively inhibiting viralDNA polymerase. Cidofovir inducesapoptosisand can be used in studies of AIDS cytomegalovirus retinitis, herpes, andcancer[1][3]. Cidofovir also has anti-orthopoxvirusand anti-variola activities[4]. |
体外研究
(In Vitro) | Cidofovir (5-100 μM, 72 hours) has antiviral activity against feline herpesvirus type-1 (FHV-1) with an IC50of 11 μM, and can reduce Crandell-Reese feline kidney cell counts in a dose-dependent manner[1].
Cidofovir (10-1000 μM, 24-120 hours) can reduce cancer cell viability and induces apoptosis[3].
Cell Cytotoxicity Assay[1] | Cell Line: | Crandell-Reese feline kidney(CRFK) cells | | Concentration: | 10-100 μM | | Incubation Time: | 72 hours | | Result: | Reduced CRFK cells by 9.1%. |
Cell Viability Assay[3] | Cell Line: | Caco-2, FTC-133, HeLa, Hep-G2, MDA-MB-231, NCI-H1975 and PC-3 cells | | Concentration: | 10-1000 μM | | Incubation Time: | 24, 48, 72, 96, 120 hours | | Result: | Resulted in a gradual decrease in tumor cell viability with time and concentration increasing and inhibited the number of FTC-133 cell clones by about 55% at 100 μM comparing to the untreated group. |
Apoptosis Analysis[3] | Cell Line: | FTC-133 cells | | Concentration: | 100 μM | | Incubation Time: | 96 hours | | Result: | Showed a significant increase in the expression of pro-apoptotic proteins, such as cytochrome c, phospho-p53 (S15) and caspase-3 by 130%, 49%, and 46%, respectively while the anti-apoptotic protein Bcl-x decreased significantly by 57% comparing to the untreated cells. |
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体内研究
(In Vivo) | Cidofovir (subcutaneous injection, 100 mg/kg, 3-6 days interval, 21 days) is highly protective against death from cowpox virus (CPV) infection at high doses in female weanling BALB/c mice[2].
| Animal Model: | Female weanling BALB/c mice infected with cowpox virus (CPV)[2] | | Dosage: | 100 mg/kg | | Administration: | Subcutaneous injection; 3-6 days interval; 21 days | | Result: | Prevented 80-100% of mouse deaths when administered on the first 4-3 days before infection.
Protected 35-50% of mice when administered on the fourth day after infection, and 10-20% when administered on the sixth day. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: H2O : 3.33 mg/mL(11.93 mM;Need ultrasonic) DMSO :< 1 mg/mL (ultrasonic;warming;heat to 80℃)(insoluble or slightly soluble) 配制储备液 | 1 mM | 3.5818 mL | 17.9090 mL | 35.8179 mL | | 5 mM | 0.7164 mL | 3.5818 mL | 7.1636 mL | | 10 mM | 0.3582 mL | 1.7909 mL | 3.5818 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 4.55 mg/mL (16.30 mM); Clear solution; Need ultrasonic and warming and heat to 60℃
*以上所有助溶剂都可在本网站选购。 |
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