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. Nr.: 2230674-01-6
- Formel: C28H36N8O6S2
- Molecular Weight:644.77
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 2230674-01-6
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Molecular Weight 644.77
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)