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普可那利 /Pleconaril {[allProObj[0].p_purity_real_show]}

货号:A479121 同义名: VP 63843;Win 63843

Pleconaril is a capsid inhibitor used previously to treat enterovirus infections. Pleconaril is effective in inhibiting replication with an IC50 of 50 nM.

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Type HazMat fee for 500 gram (Estimated)
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Pleconaril 化学结构 CAS号:153168-05-9
Pleconaril 化学结构
CAS号:153168-05-9
Pleconaril 3D分子结构
CAS号:153168-05-9
Pleconaril 化学结构 CAS号:153168-05-9
Pleconaril 3D分子结构 CAS号:153168-05-9
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Pleconaril 纯度/质量文件 产品仅供科研

货号:A479121 标准纯度: {[allProObj[0].p_purity_real_show]}
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Pleconaril 生物活性

描述 Pleconaril is a capsid inhibitor used previously to treat enterovirus infections[3]. Pleconaril binds to a hydrophobic pocket in the viral capsid inducing conformational changes, which lead to altered receptor binding and viral uncoating. Pleconaril is orally bioavailable and achieves serum concentrations in excess of those required to inhibit 90% of clinical rhino- and enteroviral isolates in vitro. It possesses the additional advantage of achieving several fold higher concentrations within the central nervous system and nasal secretions than in serum, a characteristic that is highly desirable for an antiviral targeted towards viruses known to cause central nervous system and upper respiratory tract infections. And pleconaril has demonstrated efficacy in the treatment of severe life-threatening enteroviral infections of the newborn and in immunosuppressed individuals[4]. Moreover, pleconaril dramatically reduced virus levels in target tissues of coxsackievirus serotype B3 strain M-infected animals[5].

Pleconaril 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00031512 Enteroviral Sepsis Phase 2 Completed - -
NCT00394914 Asthma Common... 展开 >> Cold Picornavirus Infection Rhinovirus 收起 << Phase 2 Completed - -
NCT00394914 - Completed - -

Pleconaril 参考文献

[1]Benschop KS, Wildenbeest JG, et al. Genetic and antigenic structural characterization for resistance of echovirus 11 to pleconaril in an immunocompromised patient. J Gen Virol. 2015 Mar;96(Pt 3):571-9.

[2]Lacroix C, Laconi S, et al. In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses. Virol J. 2015 Jul 14;12:106.

[3]Benschop KSM, Wildenbeest JG, Koen G, Minnaar RP, van Hemert FJ, Westerhuis BM, Pajkrt D, van den Broek PJ, Vossen ACTM, Wolthers KC. Genetic and antigenic structural characterization for resistance of echovirus 11 to pleconaril in an immunocompromised patient. J Gen Virol. 2015 Mar;96(Pt 3):571-579

[4]Romero JR. Pleconaril: a novel antipicornaviral drug. Expert Opin Investig Drugs. 2001 Feb;10(2):369-79

[5]Pevear DC, Tull TM, Seipel ME, Groarke JM. Activity of pleconaril against enteroviruses. Antimicrob Agents Chemother. 1999 Sep;43(9):2109-15. doi: 10.1128/AAC.43.9.2109

Pleconaril 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.11mL

2.62mL

1.31mL

26.22mL

5.24mL

2.62mL

Pleconaril 技术信息

CAS号153168-05-9
分子式C18H18F3N3O3
分子量 381.349
别名 VP 63843;Win 63843;Pleconaril, Picovir.;SR-63843;SR-263843;Picovir;APO-P001
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 105 mg/mL(275.34 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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