Cidofovir (GS 0504; HPMPC; (S)-HPMPC) dihydrate 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 dihydrate 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 dihydrate 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 dihydrate 还具有抗正痘病毒 (orthopoxvirus) 和抗天花病毒活性。
| 生物活性 | Cidofovir (GS 0504; HPMPC; (S)-HPMPC) dihydrate is an acyclic monophosphate nucleotide analogue andCMVinhibitor with antiviral activity. Cidofovir dihydrate inhibits cytomegalovirus (CMV) replication by selectively inhibiting viralDNA polymerase. Cidofovir dihydrate inducesapoptosisand can be used in studies of AIDS cytomegalovirus retinitis, herpes, andcancer[1][3]. Cidofovir dihydrate also has anti-orthopoxvirusand anti-variola activities[4]. |
体外研究
(In Vitro) | Cidofovir (5-100 μM, 72 hours) dihydrate has antiviral activity against feline herpesvirus type-1 (FHV-1) with an IC50of 11 μM, and can reduce Crandell-Reese feline kidney cells counts in a dose dependent manner[1].
Cidofovir (10-1000 μM, 24-120 hours) dihydrate 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) dihydrate 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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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