中文名 | Pirodavir |
英文名 | Pirodavir |
别名 | 吡罗达韦 4-(2-(1-(6-甲基哒嗪-3-基)哌啶-4-基)乙氧基)苯甲酸乙酯 |
英文别名 | R77975 R 77975 Pirodavir pirodavir ethyl p-(2-(1-(6-Methyl-3-pyridazinyl)-4-piperidyl)ethoxy) benzoate Ethyl 4-(2-(1-(6-methylpyridazin-3-yl)piperidin-4-yl)ethoxy)benzoate Ethyl p-[2-[1-(6-Methylpyridazin-3-yl)piperidin-4-yl]-ethoxy]benzoate Benzoic acid, 4-[2-[1-(6-Methyl-3-pyridazinyl)-4-piperidinyl]ethoxy]-, ethyl ester |
CAS | 124436-59-5 |
化学式 | C21H27N3O3 |
分子量 | 369.46 |
熔点 | 124-125℃ |
溶解度 | 氯仿 (微溶) 、DMSO (微溶) 、甲醇 (微溶) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | Off-White to Pale Beige |
靶点 | Rhinovirus |
体外研究 | Pirodavir is a potent, broad-spectrum picornavirus inhibitor. Pirodavir inhibits 80 of the 100 human rhinovirus (HRV) strains tested at a concentration of 64 ng/mL. In that same study, Pirodavir is also effective in inhibiting 16 enteroviruses, with a mean 80% inhibitory concentration (IC 80 ) of 1,300 ng/mL. Pirodavir inhibits enterovirus 71 replication with an IC 50 of 5,420 nM and an IC 90 of >13,350 nM. Pirodavir inhibits 56 rhinovirus laboratory strains and three of the clinical isolates tested. Pirodavir inhibits 59% of the serotypes and isolates with IC 50 s of <100 nM. Pirodavir concentrations of 16 and 4μg/mL reduces cell growth by 66% (s.e.m. 0.75) and 28% (s.e.m. 0.25), respectively. Lower concentrations (1μg/mL) of Pirodavir are not inhibitory for cell growth. The 50% cytotoxic concentration of pirodavir for logarithmic cell growth at 37°C is 7μg/mL. Under the conditions of the antiviral assay (confluent HeLa cells at 33°C), the 50% cytotoxic concentration is >50μg/mL. |
参考资料 展开查看 | 1: Lacroix C, Laconi S, Angius F, Coluccia A, Silvestri R, Pompei R, Neyts J, Leyssen P. In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses. Virol J. 2015 Jul 14;12:106. doi: 10.1186/s12985-015-0330-4. PubMed PMID: 26169596; PubMed Central PMCID: PMC4501209. 2: Bernard A, Lacroix C, Cabiddu MG, Neyts J, Leyssen P, Pompei R. Exploration of the anti-enterovirus activity of a series of pleconaril/pirodavir-like compounds. Antivir Chem Chemother. 2015 Apr;24(2):56-61. doi: 10.1177/2040206615589035. Epub 2015 Jun 11. PubMed PMID: 26071135. 3: Barnard DL, Hubbard VD, Smee DF, Sidwell RW, Watson KG, Tucker SP, Reece PA. In vitro activity of expanded-spectrum pyridazinyl oxime ethers related to pirodavir: novel capsid-binding inhibitors with potent antipicornavirus activity. Antimicrob Agents Chemother. 2004 May;48(5):1766-72. PubMed PMID: 15105133; PubMed Central PMCID: PMC400527. 4: Rombaut B, Andries K, Boeyé A. Stabilisation of poliovirus with pirodavir. Dev Biol Stand. 1996;87:173-80. PubMed PMID: 8854015. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.707 ml | 13.533 ml | 27.067 ml |
5 mM | 0.541 ml | 2.707 ml | 5.413 ml |
10 mM | 0.271 ml | 1.353 ml | 2.707 ml |
5 mM | 0.054 ml | 0.271 ml | 0.541 ml |
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