产品说明书

Pleconaril

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Chemical Structure| 153168-05-9 同义名 : VP 63843;Win 63843;Pleconaril, Picovir.;SR-63843;SR-263843;Picovir;APO-P001
CAS号 : 153168-05-9
货号 : A479121
分子式 : C18H18F3N3O3
纯度 : 99%+
分子量 : 381.349
MDL号 : MFCD00923611
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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

动物实验配方:
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].
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 - -
实验方案
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

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