N-0385
N-0385 is an antiviral agent active against SARS-CoV-2 and its Omicron subvariants. N-0385 acts on factors such as TMPRSS2 to block viral entry, reduce infection, regulate metabolism and inhibit inflammatory responses. N-0385 reduces SARS-CoV-2-induced mortality, weight loss, pulmonary pathological changes and cellular damage in animal models. N-0385 can be used in research related to coronavirus infections.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2230674-01-6
- 分子式: C28H36N8O6S2
- 分子量:644.77
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
N-0385 potently inhibits SARS-CoV-2 infection in human lung epithelial cells (IC50 = 12.3 nM) and Calu-3 cells by targeting TMPRSS2[1].
N-0385 (1 μM; 3 h pretreatment, 72 h VLP incubation) potently inhibits TMPRSS2-dependent entry of Omicron subvariant (BA.1, BA.2, BA.5) and pre-Omicron SARS-CoV-2 VLPs into human Calu-3 lung cells[2].
N-0385 (3 h pretreatment, 48 h viral infection) exhibits broad-spectrum, low nanomolar antiviral activity against SARS-CoV-2 Omicron subvariants (BA.1, BA.2, BA.5, BQ.1.1, XBB.1.5, EG.5.1, BA.2.86) in human Calu-3 lung cells, with EC50 values ranging from 2.0 nM to 29.1 nM[2].
N-0385 (20 nM; 3 h pretreatment) robustly inhibits SARS-CoV-2 Omicron BA.5 infection in normal human bronchial epithelial cells, achieving 85.7% inhibition at a concentration of 20 nM[2].
N-0385 (3 h pretreatment, 48 h viral infection) acts synergistically with Nirmatrelvir (HY-138687) and Remdesivir (HY-104077) to inhibit SARS-CoV-2 Omicron subvariants (BA.1, BA.2, BA.5) in human Calu-3 lung cells, with Loewe synergy scores ranging from 19.94 to 49.23[2].
N-0385 forms tight, specific binding interactions with human ACE2, DPP4, IL-10, NLRP3, TLR7, and TMPRSS2 proteins via hydrogen bonding, hydrophobic interactions, ionic bonding, and pi-based interactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
化学情報
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CAS 番号 2230674-01-6
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分子量 644.77
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分子式 C28H36N8O6S2
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SMILES
NC(CC[C@H](NS(C)(=O)=O)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CCCNC(N)=N)C(C2=NC3=CC=CC=C3S2)=O)=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
純度とドキュメンテーション
参考文献
[1]. Cao JF, et al. Mechanism of N-0385 blocking SARS-CoV-2 to treat COVID-19 based on molecular docking and molecular dynamics. Frontiers in microbiology. 2022;13:1013911. [Content Brief]
[2]. Pérez-Vargas J, et al. Nanomolar anti-SARS-CoV-2 Omicron activity of the host-directed TMPRSS2 inhibitor N-0385 and synergistic action with direct-acting antivirals. Antiviral research. 2024 May;225:105869. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)