954389-09-4
954389-09-4 structure
- Name: JTK-853
- Chemical Name: (2R)-4-(5-cyclopropyl-[1,3]thiazolo[4,5-d]pyrimidin-2-yl)-N-[[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]-1-[4-(trifluoromethyl)phenyl]sulfonylpiperazine-2-carboxamide
- CAS Number: 954389-09-4
- Molecular Formula: C28H23F7N6O4S2
- Molecular Weight: 704.63900
- Catalog: Signaling Pathways Anti-infection HCV
- Create Date: 2016-03-19 03:04:27
- Modify Date: 2024-01-02 14:55:35
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JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.
| Name | (2R)-4-(5-cyclopropyl-[1,3]thiazolo[4,5-d]pyrimidin-2-yl)-N-[[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]-1-[4-(trifluoromethyl)phenyl]sulfonylpiperazine-2-carboxamide |
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| Synonyms |
UNII-WDX8QQD13B
JT1 3vqs JTK-853 |
| Description | JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively. |
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| Related Catalog | |
| Target |
HCV polymerase[1] EC50: 0.38 μM (1a H77 HCV), 0.035 μM (1b Con1 HCV)[1] |
| In Vitro | JTK-853 is a novel, non-nucleoside Hepatitis C Virus Polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively. When JTK-853 is incubated with the replicon cells for 48 h, it shows antiviral activity against genotype 1a H77 and 1b Con1 replicon cells with EC90 values of 6.5±0.5 and 0.34±0.05 µM, respectively. At 10 µM, JTK-853 induces apparent Huh-7.5 cell death in 2-week culture. JTK-853 suppresses the drug-resistant colony formation in the genotype 1a replicon cells, and the numbers of JTK-853-resistant colonies are much lower than those of GS-9190-resistant colonies for both genotypes[1]. |
| Cell Assay | For the determination of cytotoxicity of JTK-853, the Huh-7.5 cells are treated with JTK-853 for 2 weeks. The thumb pocket NNI-B and NS5Ai are added at 100 µM and 100 nM, respectively. JTK-853 is added at 10 µM. JTK-853-containing medium is changed twice a week. Two weeks after the culture, the cells are stained with crystal violet [1% (v/v) in methanol], and then lysed by the lysis buffer. The cytotoxicity is determined as a measurement of OD 595 nm of the cell lysates[1]. |
| References |
| Molecular Formula | C28H23F7N6O4S2 |
|---|---|
| Molecular Weight | 704.63900 |
| Exact Mass | 704.11100 |
| PSA | 157.73000 |
| LogP | 7.14010 |
| Storage condition | 2-8℃ |