Nirmatrelvir (PF-07321332)

製品コードS9866 バッチS986602

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C23H32F3N5O4
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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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>

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme kinetics assay
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
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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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