受注:045-509-1970 |
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Synonyms | TMC125, R-165335 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H15BrN6O |
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分子量 | 435.28 | CAS No. | 269055-15-4 | |
Solubility (25°C)* | 体外 | DMSO | 87 mg/mL (199.87 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. |
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in vitro | Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. [1] [2] |
in vivo | Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group. [3] |
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Data from [Data independently produced by , , Biochemistry, 2016, 55(28):3864-73]
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
Time-Course Transcriptome Analysis for Drug Repositioning in Fusobacterium nucleatum-Infected Human Gingival Fibroblasts. [ Front Cell Dev Biol, 2019, 7:204] | PubMed: 31608279 |
HIV-1 Subtype C with PYxE Insertion Has Enhanced Binding of Gag-p6 to Host Cell Protein ALIX and Increased Replication Fitness. [ J Virol, 2019, 93(9)] | PubMed: 30760577 |
Antiretroviral potency of 4'-ethnyl-2'-fluoro-2'-deoxyadenosine, tenofovir alafenamide and second-generation NNRTIs across diverse HIV-1 subtypes. [ J Antimicrob Chemother, 2018, 73(10):2721-2728] | PubMed: 30053052 |
Discovery of dapivirine, a nonnucleoside HIV-1 reverse transcriptase inhibitor, as a broad-spectrum antiviral against both influenza A and B viruses [Hu Y, et al. Antiviral Res, 2017, 145:103-113] | PubMed: 28778830 |
Detection of treatment-resistant infectious HIV after genome-directed antiviral endonuclease therapy. [ Antiviral Res, 2016, 126:90-8] | PubMed: 26718067 |
Conformational Plasticity of the NNRTI-Binding Pocket in HIV-1 Reverse Transcriptase: A Fluorine Nuclear Magnetic Resonance Study [Sharaf NG, et al. Biochemistry, 2016, 55(28):3864-73] | PubMed: 27163463 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。