Pleconaril

Names

[ Name ]:
Pleconaril

[Synonym ]:
Pleconaril
Picovir
Pleconarilis

Biological Activity

[Description]:

Pleconaril is a capsid inhibitor used previously to treat enterovirus infections. Pleconaril is effective in inhibiting replication with an IC50 of 50 nM.Target: enterovirusPleconaril is a capsid inhibitor designed to dock within a hydrophobic pocket formed by the capsid proteins VP1, VP3 and VP2. Pleconaril leads to stiffening of the capsid structure,preventing RNA release into the cell. Pleconaril has been used as treatment on a compassionateuse basis in neonates and immunodeficient patients with severe EV infections.

[Related Catalog]:

Signaling Pathways >> Anti-infection >> Enterovirus

Research Areas >> Infection

[References]

[1]. Benschop KS, 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, et al. http://www.ncbi.nlm. In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses. Virol J. 2015 Jul 14;12:106.

[Related Small Molecules]

Pirodavir | Pocapavir

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
481.2±55.0 °C at 760 mmHg

[ Melting Point ]:
61-62°

[ Molecular Formula ]:
C₁₈H₁₈F₃N₃O₃

[ Molecular Weight ]:
381.349

[ Flash Point ]:
244.8±31.5 °C

[ Exact Mass ]:
381.130035

[ PSA ]:
74.18000

[ LogP ]:
5.77

[ Appearance of Characters ]:
white to beige

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.509

[ Storage condition ]:
room temp

[ Water Solubility ]:
DMSO: ≥10mg/mL (warmed)

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H413

[ Precautionary Statements ]:
P301 + P310

[ Hazard Codes ]:
T

[ Risk Phrases ]:
25

[ Safety Phrases ]:
45

[ RIDADR ]:
UN 2811 6.1 / PGIII

Articles

Molecular mechanism of a specific capsid binder resistance caused by mutations outside the binding pocket.

Antiviral Res. 123 , 138-45, (2015)

Enteroviruses cause various acute and chronic diseases. The most promising therapeutics for these infections are capsid-binding molecules. These can act against a broad spectrum of enteroviruses, but ...

Microscopic determination of drug solubility in plasma and calculation of injection rates with a plasma circulatory model to prevent precipitation on intravenous injection.

J. Pharm. Biomed. Anal. 13(9) , 1189-93, (1995)