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Synonyms | MK-4482 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C13H19N3O7 |
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分子量 | 329.31 | CAS No. | 2349386-89-4 | |
Solubility (25°C)* | 体外 | DMSO | 66 mg/mL (200.41 mM) | |
Ethanol | 33 mg/mL (100.2 mM) | |||
Water | 17 mg/mL (51.62 mM) | |||
* <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 | Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
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in vitro | EIDD-2801 is an orally bioavailable NHC-prodrug. NHC is potently antiviral against SARS-CoV-2, MERS-CoV and SARS-CoV in primary human epithelial cell cultures without cytotoxicity. NHC is effective against remdesivir (RDV)-resistant vi-rus and multiple distinct zoonotic CoV. NHC antiviral activity is associated with increased viral mutation rates.[1] |
in vivo | EIDD-2801 is efficiently hydrolyzed in vivo after absorption, resulting in detection of only free NHC in plasma.[2] Therapeutic EIDD-2801 is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit is dependent on the time of initiation post-infection. EIDD-2801 robustly reduces MERS-CoV infectious titers, viral RNA, and pathogenesis under both prophylactic and early therapeutic conditions.[1] |
細胞アッセイ | 細胞株 | Huh-7 & Caco-2 cells |
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濃度 | IC50 values of 2.84, 25.4, and 1.62 µM for hCoV-229E, -NL63, and -OC43, respectively | |
反応時間 | 7 days | |
実験の流れ | ||
動物実験 | 動物モデル | 20-29 week old SPF C57BL/6J mice, 10-14 week old C57BL/6J hDPP4 mice |
投薬量 | 50 mg/kg, 150 mg/kg, 500 mg/kg | |
投与方法 | Oral gavage |
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A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry [ Cell, 2023, 186(4):850-863.e16] | PubMed: 36803605 |
Preclinical development of kinetin as a safe error-prone SARS-CoV-2 antiviral able to attenuate virus-induced inflammation [ Nat Commun, 2023, 14(1):199] | PubMed: 36639383 |
Efferocytosis of SARS-CoV-2-infected dying cells impairs macrophage anti-inflammatory functions and clearance of apoptotic cells [ Elife, 2022, 11e74443] | PubMed: 35666101 |
Immunodetection assays for the quantification of seasonal common cold coronaviruses OC43, NL63, or 229E infection confirm nirmatrelvir as broad coronavirus inhibitor [ Antiviral Res, 2022, 203:105343] | PubMed: 35598779 |
In vitro and in vivo efficacy of a novel nucleoside analog H44 against Crimean-Congo hemorrhagic fever virus [ Antiviral Res, 2022, 199:105273] | PubMed: 35257725 |
The MEK1/2 Inhibitor ATR-002 (Zapnometinib) Synergistically Potentiates the Antiviral Effect of Direct-Acting Anti-SARS-CoV-2 Drugs [ Pharmaceutics, 2022, 14(9)1776] | PubMed: 36145524 |
Use of Human Lung Tissue Models for Screening of Drugs against SARS-CoV-2 Infection [ Viruses, 2022, 14(11)2417] | PubMed: 36366514 |
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 |
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。