化学信息:
化学名
|
ethyl 4-[2-[1-(6-methylpyridazin-3-yl)piperidin-4-yl]ethoxy]benzoate
|
|
简称
|
Pirodavir
|
别名
|
R-77975, R77975, R 77975
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中文名
|
吡罗达韦
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化学式
|
C21H27N3O3
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分子量
|
396.46
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CAS号
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124436-59-5
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO67mg/ml; Ethanol7mg/ml
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溶液配制
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5mg加入1.26ml DMSO,或者每3.96mg加入1ml DMSO,配制成10mM溶液。SC3274-10mM用DMSO配制。
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生物信息:
产品描述
|
Pirodavir (R 77975) is the prototype of a novel class of broad-spectrum antipicornavirus compounds; potent human rhinovirus (HRV) capsid-binding inhibitor.
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信号通路
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Anti-infection
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靶点
|
broad-spectrum antipicornavirus
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capsid-binding
|
-
|
-
|
-
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IC50
|
-
|
-
|
-
|
-
|
-
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体外研究
|
R-77975's predecessor, R 61837, a substituted phenyl-pyridazinamine, was effective in inhibiting 80% of 100 serotypes tested (EC80) at concentrations above 32 micrograms/ml, pirodavir inhibits the same percentage of viruses at 0.064 micrograms/ml. Pirodavir is also effective in inhibiting 16 enteroviruses, with an EC80 of 1.3 micrograms/ml. Pirodavir acts at an early stage of the viral replication cycle (up to 40 min after infection) and reduces the yield of selected rhinoviruses 1,000- to 100,000-fold in a single round of replication.
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体内研究
|
Adults with symptoms of < or =2 days' duration were randomly assigned to intranasal sprays of pirodavir (2mg per treatment) or placebo six times daily for 5 days. In people with laboratory-documented rhinovirus colds (53 in the pirodavir group, 55 in the placebo group), no significant differences in the resolution of respiratory symptoms were apparent between the groups. The median duration of illness was 7 days in each group. Similarly, scores for individual symptoms found no differences in favor of pirodavir during or after treatment.
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临床实验
|
N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
酶活性检测实验
|
方法
|
N/A
|
细胞实验
|
细胞系
|
N/A
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浓度
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N/A
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处理时间
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N/A
|
方法
|
N/A
|
动物实验
|
动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献:
1. Barnard DL, Hubbard VD, Smee DF. Antimicrob Agents Chemother. 2004 May, 48(5), 1766-72.
2. Andries K, Dewindt B, Snoeks J. Antimicrob Agents Chemother. 1992 Jan, 36(1), 100-7.
3. Hayden FG, Hipskind GJ, Woerner DH. Antimicrob Agents Chemother. 1995 Feb, 39(2), 290-4.
包装清单:
产品编号
|
产品名称
|
包装
|
SC3274-10mM
|
Pirodavir (HRV capsid-binding抑制剂)
|
10mM×0.2ml
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SC3274-5mg
|
Pirodavir (HRV capsid-binding抑制剂)
|
5mg
|
SC3274-25mg
|
Pirodavir (HRV capsid-binding抑制剂)
|
25mg
|
—
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说明书
|
1份
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保存条件:
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
本产品对人体有刺激性,操作时请小心,并注意适当防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。