受注:045-509-1970 |
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Synonyms | R278474, TMC278, DB08864 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H18N6 |
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分子量 | 366.42 | CAS No. | 500287-72-9 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 73 mg/mL (199.22 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection. |
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in vitro | Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. [1] Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development. [2] |
in vivo | After iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. [1] |
特徴 | Approved anti-HIV drug with longer half-life and reduced side-effect profile than older NNRTIs. |
動物実験 | 動物モデル | Sprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey. |
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投薬量 | 4 mg/kg ( rat); 1.25 mg/kg (other species) | |
投与方法 | i.v., p.o. |
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Chemical inhibition of DPP9 sensitizes the CARD8 inflammasome in HIV-1-infected cells [ Nat Chem Biol, 2023, 19(4):431-439] | PubMed: 36357533 |
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021] | PubMed: 35019724 |
Biodegradable polymeric solid implants for ultra-long-acting delivery of single or multiple antiretroviral drugs [ Int J Pharm, 2021, 605:120844] | PubMed: 34216767 |
High levels of LINE-1 transposable elements expressed in Kaposi's sarcoma-associated herpesvirus-related primary effusion lymphoma [ Oncogene, 2020, 10.1038/s41388-020-01549-9] | PubMed: 33188297 |
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536] | PubMed: 33346662 |
Effect of HIV infection and antiretroviral therapy on immune cellular functions. [ JCI Insight, 2019, 4(12)] | PubMed: 31217351 |
Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation. [ Structure, 2019, 27(10):1581-1593] | PubMed: 31471129 |
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 |
Nonnucleoside Reverse Transcriptase Inhibitor Hypersusceptibility and Resistance by Mutation of Residue 181 in HIV-1 Reverse Transcriptase. [ Antimicrob Agents Chemother, 2019, 63(8)] | PubMed: 31160281 |
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。