N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide

Modify Date: 2024-04-06 18:24:48

N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide Structure
N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide structure
Common Name N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide
CAS Number 351438-49-8 Molecular Weight 417.408
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C19H14F3N5OS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide


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].

 Names

Name 2-[(5-Methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]-N-[3-(trifluoromethyl)phenyl]acetamide
Synonym More Synonyms

  Biological Activity

Description 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].
Related Catalog
Target

EC50: 10 nM (PV-1), 26 nM (PV-2), 218 nM (PV-3)[1]

In Vitro 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].
References

[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.

[2]. Tijsma A. Antiviral strategies against polio and other enteroviruses. 2018.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Molecular Formula C19H14F3N5OS
Molecular Weight 417.408
Exact Mass 417.087128
LogP 4.29
Index of Refraction 1.674

 Synonyms

2-[(5-Methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]-N-[3-(trifluoromethyl)phenyl]acetamide
Acetamide, 2-[(5-methyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-[3-(trifluoromethyl)phenyl]-
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Price: ¥1200/5 mg

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