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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- CAS No.: 2230674-01-6
- 화학식: C28H36N8O6S2
- 분자량:644.77
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
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.
In Vivo
Chemical Information
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CAS No. 2230674-01-6
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분자량 644.77
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
N-0385 Related Classifications
HY-187788 Related Classifications
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