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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C23H32F3N5O4 |
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分子量 | 499.53 | CAS No. | 2628280-40-8 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (200.18 mM) | |
Ethanol | 100 mg/mL (200.18 mM) | |||
Water | 2 mg/mL (4.0 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 | Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme. |
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in vitro | Nirmatrelvir (PF-07321332) is a reversible covalent inhibitor of SARS-CoV-2 main protease (M<sup>pro</sup>, also known as 3CL protease), and ki is 3.11 nM.
PF- 07321332 directly binds to the catalytic cysteine (Cys145) residue of the enzyme.<sup><a class="sref" href="#s_ref">[1]</a></sup>
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キナーゼアッセイ | Enzyme kinetics assay | |
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Test compounds and SARS-CoV-2 Mpro enzyme were incubated at a 1:1 molar ratio of 2 μM compound and 2 μM enzyme in assay buffer for 20 minutes. The mixture was then diluted 50-fold into assay buffer followed by a transfer of 5 μl to wells of a black low volume 384-well assay plate. Enzyme activity was monitored on a BMG Pherastar at Ex/Em of 340 nm/460 nm after addition of 5 μl 60 μM peptide substrate. Final reaction conditions were 20 nM enzyme with 20 nM compound and 30 μM peptide substrate. | ||
細胞アッセイ | 細胞株 | HCoV-229E in Huh-7 cells |
濃度 | 0.62 µM | |
反応時間 | 2 days | |
実験の流れ | hCoV-229E experiments were performed on Huh-7 cells at an MOI of 0.002 and infection determined by in-cell ELISA 2 days later |
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動物実験 | 動物モデル | Female C57BL/6 Cg-Tg2Prlmn/J mice |
投薬量 | 20 mg/kg | |
投与方法 | Oral |
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The host-targeted antiviral drug Zapnometinib exhibits a high barrier to the development of SARS-CoV-2 resistance [ Antiviral Res, 2024, 225:105840] | PubMed: 38438015 |
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062] | PubMed: 37047038 |
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 |
Autoprocessing and oxyanion loop reorganization upon GC373 and nirmatrelvir binding of monomeric SARS-CoV-2 main protease catalytic domain [ Commun Biol, 2022, 5(1):976] | PubMed: 36114420 |
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 |
PF-07321332 (Nirmatrelvir) Does Not Interact with Human ENT1 or ENT2: Implications for COVID-19 Patients [ Clin Transl Sci, 2022, 10.1111/cts.13292] | PubMed: 35505633 |
Virologic and Immunologic Characterization of COVID-19 Recrudescence after Nirmatrelvir/Ritonavir Treatment [ Res Sq, 2022, rs.3.rs-1662783] | PubMed: 35611335 |
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。