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Cidofovir Dihydrate

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Chemical Structure| 149394-66-1 同义名 : (S)-HPMPC dihydrate;GS 0504 dihydrate;Cidofovir hydrate;HPMPC dihydrate
CAS号 : 149394-66-1
货号 : A102690
分子式 : C8H18N3O8P
纯度 : 98%
分子量 : 315.218
MDL号 : MFCD16556167
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Cidofovir is a synthetic nucleotide analog with potent antiviral activity against a wide range of herpes viruses. Cidofovir dihydrate (1-((S)-3-Hydroxy-2-(phosphonomethoxy)propyl) cytosine dihydrate) is the active intracellular metabolite of cidofovir that can inhibit cytomegalovirus DNA polymerase[1]. 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[2].
作用机制 Cidofovir dihydrate is the active form of cidofovir and it inhibits viral DNA polymerases as an acyclic nucleoside phosphonate[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.86mL

3.17mL

1.59mL

31.72mL

6.34mL

3.17mL

参考文献

[1]Davis JL, Taskintuna I, et al. Iritis and hypotony after treatment with intravenous cidofovir for cytomegalovirus retinitis. Arch Ophthalmol. 1997;115(6):733-7.

[2]de Oliveira CB, Stevenson D, et al. Evaluation of Cidofovir (HPMPC, GS-504) against adenovirus type 5 infection in vitro and in a New Zealand rabbit ocular model. Antiviral Res. 1996;31(3):165-72.

[3]Mendel DB, Barkhimer DB, et al. Biochemical basis for increased susceptibility to Cidofovir of herpes simplex viruses with altered or deficient thymidine kinase activity. Antimicrob Agents Chemother. 1995;39(9):2120-2.