Pirodavir

Category	Enterovirus (EV)
CAS	124436-59-5
Description	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. Adults with symptoms of < or = 2 days' duration were randomly assigned to intranasal sprays of pirodavir (2 mg 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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Product Information

Synonyms	R 77975; R-77975; R77975; R77,975; R 77,975; R-77,975; Pirodavir.
Molecular Weight	369.46
Molecular Formula	C21H27N3O3
Canonical SMILES	CCOC(=O)C1=CC=C(C=C1)OCCC2CCN(CC2)C3=NN=C(C=C3)C
InChI	InChI=1S/C21H27N3O3/c1-3-26-21(25)18-5-7-19(8-6-18)27-15-12-17-10-13-24(14-11-17)20-9-4-16(2)22-23-20/h4-9,17H,3,10-15H2,1-2H3
InChIKey	KCHIOGFOPPOUJC-UHFFFAOYSA-N
Boiling Point	572.0±40.0 °C at 760 mmHg
Melting Point	124-125°C
Flash Point	299.8±27.3 °C
Purity	>98%
Density	1.1±0.1 g/cm3
Solubility	In Vitro: 10 mM in DMSO
Appearance	Light yellow to yellow (Solid)
Storage	Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month
Complexity	446
Exact Mass	369.20524173
Index Of Refraction	1.554
In Vitro	Pirodavir inhibits 80 of the 100 human rhinovirus (HRV) strains tested at a concentration of 64 ng/mL. Pirodavir is also effective in inhibiting 16 enteroviruses, with a mean 80% inhibitory concentration (IC80) of 1,300 ng/mL. Pirodavir inhibits enterovirus 71 replication with an IC50 of 5,420 nM and an IC90 of >13,350 nM. Pirodavir inhibits 59% of the serotypes and isolates with IC50s of <100 nM. Pirodavir concentrations of 16 and 4 μg/mL reduces cell growth by 66% and 28%, respectively. Lower concentrations (1 μg/mL) of Pirodavir are not inhibitory for cell growth. The 50% cytotoxic concentration of pirodavir for logarithmic cell growth at 37°C is 7 μg/mL. Under the conditions of the antiviral assay (confluent HeLa cells at 33°C), the 50% cytotoxic concentration is >50 μg/mL.
PSA	64.55000
Target	Enterovirus
Vapor Pressure	0.0±1.6 mmHg at 25°C
XLogP3-AA	3.7