H1PVAT

• CAT Number: I042956
• CAS Number: 351438-49-8
• Molecular Formula: C19H14F3N5OS
• Molecular Weight: 417.41
• Purity: ≥95%
• Synonyms: N-(4-cyanophenyl)-5-thiophen-2-yl-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide
• InChI: InChI=1S/C19H14F3N5OS/c20-19(21,22)16-8-13(15-2-1-7-29-15)25-17-9-14(26-27(16)17)18(28)24-12-5-3-11(10-23)4-6-12/h1-7,9,13,16,25H,8H2,(H,24,28)
• InChIKey: FITXCLRWDSMQLY-UHFFFAOYSA-N
• SMILES: C1C(NC2=CC(=NN2C1C(F)(F)F)C(=O)NC3=CC=C(C=C3)C#N)C4=CC=CS4

H1PVAT is a potent and selective inhibitor of poliovirus serotypes (PV-1, PV-2, PV-3), and inhibits early stage of the replication. H1PVAT interacts with viral capsid directly and protects PV against heat inactivation[1][2].
H1PVAT (10-218 nM; 24-48 h) inhibits poliovirus strain Sabin replication in a dose-dependent manner, with EC50s of 10 nM (PV-1), 26 nM (PV-2) and 218 nM (PV-3), respectively[1].
H1PVAT (30 min prior to or 1 h after PV-1 infection; 7 h) inhibits an early stage of viral replication , and only H1PVAT is administered prior to infection results reduction (>99.9%) in intracellular viral RNA levels[1].
H1PVAT (50 μM; 2 min) protects PV against heat inactivation with the 50% thermal inactivation temperature increased to 52.6 ℃ and 50.8 ℃, which suggests a direct interaction between the viral capsid and H1PVAT[1].

Reference

[1]. Tijsma A, et al. H1PVAT is a novel and potent early-stage inhibitor of poliovirus replication that targets VP1. Antiviral Res. 2014 Oct;110:1-9.
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[2]. Tijsma A. Antiviral strategies against polio and other enteroviruses. 2018.