JTK-853
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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- CAS 番号: 954389-09-4
- 分子式: C28H23F7N6O4S2
- 分子量:704.64
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
HCV polymerase[1] EC50: 0.38 μM (1a H77 HCV), 0.035 μM (1b Con1 HCV)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 954389-09-4
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分子量 704.64
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分子式 C28H23F7N6O4S2
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SMILES
O=C([C@@H]1N(S(=O)(C2=CC=C(C(F)(F)F)C=C2)=O)CCN(C3=NC4=NC(C5CC5)=NC=C4S3)C1)NCC6=CC=C(OC(F)(F)F)C(F)=C6
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)