受注:045-509-1970 |
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Synonyms | EBP 520, SCH 503034 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H45N5O5 |
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分子量 | 519.68 | CAS No. | 394730-60-0 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (192.42 mM) | |
Ethanol | 100 mg/mL (192.42 mM) | |||
Water | 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 | Boceprevir (EBP 520, SCH 503034) is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1. |
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in vitro | Treatment with NLRP3 Inflammasome Inhibitor I significantly limits IL-1β release after LPS and ATP challenge. NLRP3 Inflammasome Inhibitor I is not a caspase-1 inhibitor[1]. |
in vivo | The small molecule NLRP3 Inflammasome Inhibitor I, an intermediate substrate in the glyburide synthesis free of the cyclohexylurea moiety, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism[1]. |
細胞アッセイ | 細胞株 | J774A.1 cells |
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濃度 | 400 μM | |
反応時間 | 30 mins | |
実験の流れ | J774A.1 cells, a murine macrophage cell line, are plated at 5×104 cells/well in a 96 multiwell plate for 24 hours in RPMI medium supplemented with 10% of fetal bovine serum (FBS). The cells are primed with Escherichia coli 0111:B4 LPS(1 μg/ml) for 4 hours and then ATP (5 mM) for 30 minutes to induce the NLRP3 inflammasome formation. The supernatants are collected and levels of IL-1β are measured with a mouse IL-1β ELISA kit. To test the inhibitory effects of 16673-34-0 on NLRP3 inflammasome activation, cells are co-treated with 16673-34-0 (400μM) or Glyburide (400μM) at the time of ATP for 30 minutes, and IL-1β levels are used as read-out. | |
動物実験 | 動物モデル | CD1 mice |
投薬量 | 100 mg/kg | |
投与方法 | i.p. |
Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity [ Eur J Med Chem, 2024, 268:116202] | PubMed: 38394929 |
Discovery of novel SARS-CoV-2 inhibitors targeting the main protease Mpro by virtual screenings and hit optimization [ Antiviral Res, 2022, 204:105350] | PubMed: 35688349 |
From Repurposing to Redesign: Optimization of Boceprevir to Highly Potent Inhibitors of the SARS-CoV-2 Main Protease [ Molecules, 2022, 27(13)4292] | PubMed: 35807537 |
Integrative multiomics and in silico analysis revealed the role of ARHGEF1 and its screened antagonist in mild and severe COVID-19 patients [ J Cell Biochem, 2022, 10.1002/jcb.30213] | PubMed: 35037717 |
BRET-Based Self-Cleaving Biosensors for SARS-CoV-2 3CLpro Inhibitor Discovery [ Microbiol Spectr, 2022, 10(4):e0255921] | PubMed: 35758897 |
Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture [ Cell Rep, 2021, 35(7):109133] | PubMed: 33984267 |
Ugonin J Acts as a SARS-CoV-2 3C-like Protease Inhibitor and Exhibits Anti-inflammatory Properties [ Front Pharmacol, 2021, 12:720018] | PubMed: 34512347 |
Pre-Steady-State Kinetics of the SARS-CoV-2 Main Protease as a Powerful Tool for Antiviral Drug Discovery [ Front Pharmacol, 2021, 12:773198] | PubMed: 34938188 |
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors [ Viruses, 2021, 13(2)173] | PubMed: 33498923 |
Characterization of fluorescent probe substrates to develop an efficient high-throughput assay for neonatal hepatic CYP3A7 inhibition screening [ Sci Rep, 2021, 11(1):19443] | PubMed: 34593846 |
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。