CBS1194
CBS1194 is a selective group 2 influenza virus inhibitor. CBS1194 binds to the pocket region adjacent to the HA fusion peptide, generates steric hindrance, and blocks the low pH-induced HA conformational rearrangement required for membrane fusion. CBS1194 exerts inhibitory activity in the early stage of viral infection and can inhibit HA-mediated hemolysis. CBS1194 serves as a lead compound for the development of improved influenza virus entry inhibitors. CBS1194 is applicable to studies related to influenza virus infection.
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- CAS. Nr.: 901259-15-2
- Formel: C22H19BrN4O2
- Molecular Weight:451.32
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | EC50 |
0.25 μM
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Inhibition of H7 HA-bearing pseudovirus (group 2 influenza) infection in human A549 cells measured by luciferase-based pseudovirus infection assay after 48 h incubation.
Inhibition of H7 HA-bearing pseudovirus (group 2 influenza) infection in human A549 cells measured by luciferase-based pseudovirus infection assay after 48 h incubation.
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33428962 |
| A549 | EC50 |
49.30 μM
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Inhibition of H5 HA-bearing pseudovirus (group 1 influenza) infection in human A549 cells measured by luciferase-based pseudovirus infection assay after 48 h incubation.
Inhibition of H5 HA-bearing pseudovirus (group 1 influenza) infection in human A549 cells measured by luciferase-based pseudovirus infection assay after 48 h incubation.
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33428962 |
| A549 | EC50 |
54.53 μM
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Inhibition of Lassa virus pseudovirus infection in human A549 cells measured by luciferase-based pseudovirus infection assay after 48 h incubation.
Inhibition of Lassa virus pseudovirus infection in human A549 cells measured by luciferase-based pseudovirus infection assay after 48 h incubation.
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33428962 |
| MDCK | EC50 |
3.17 μM
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Inhibition of group 2 influenza A/rhea/North Carolina/1993 (H7N1) replication in canine MDCK cells measured by cytopathic effect (CPE) inhibition assay with CCK-8 viability readout after 72 h incubation.
Inhibition of group 2 influenza A/rhea/North Carolina/1993 (H7N1) replication in canine MDCK cells measured by cytopathic effect (CPE) inhibition assay with CCK-8 viability readout after 72 h incubation.
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33428962 |
| MDCK | EC50 |
1.60 μM
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Inhibition of group 2 influenza A/Hong Kong/1/1968 (H3N2) replication in canine MDCK cells measured by cytopathic effect (CPE) inhibition assay with CCK-8 viability readout after 72 h incubation.
Inhibition of group 2 influenza A/Hong Kong/1/1968 (H3N2) replication in canine MDCK cells measured by cytopathic effect (CPE) inhibition assay with CCK-8 viability readout after 72 h incubation.
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33428962 |
| MDCK | EC50 |
0.74 μM
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Inhibition of group 2 influenza A/Brisbane/10/2007 (H3N2) replication in canine MDCK cells measured by cytopathic effect (CPE) inhibition assay with CCK-8 viability readout after 72 h incubation.
Inhibition of group 2 influenza A/Brisbane/10/2007 (H3N2) replication in canine MDCK cells measured by cytopathic effect (CPE) inhibition assay with CCK-8 viability readout after 72 h incubation.
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33428962 |
| MDCK | EC50 |
0.36 μM
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Inhibition of group 2 influenza reporter virus A/NY-r19-GLuc (H3N2) replication in canine MDCK cells measured by Gaussia luciferase-based reporter virus infection assay after 24 h post-inoculum incubation.
Inhibition of group 2 influenza reporter virus A/NY-r19-GLuc (H3N2) replication in canine MDCK cells measured by Gaussia luciferase-based reporter virus infection assay after 24 h post-inoculum incubation.
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33428962 |
| MDCK | EC90 |
2.8 μM
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90% inhibition of wild-type influenza A/Hong Kong/1/1968 (H3N2) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
90% inhibition of wild-type influenza A/Hong Kong/1/1968 (H3N2) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
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33428962 |
| MDCK | EC90 |
13.3 μM
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90% inhibition of influenza A/Hong Kong/1/1968 (H3N2) escape mutant M1 (HA1 T30A) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
90% inhibition of influenza A/Hong Kong/1/1968 (H3N2) escape mutant M1 (HA1 T30A) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
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33428962 |
| MDCK | EC90 |
17.4 μM
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90% inhibition of influenza A/Hong Kong/1/1968 (H3N2) escape mutant M2 (HA2 K117N) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
90% inhibition of influenza A/Hong Kong/1/1968 (H3N2) escape mutant M2 (HA2 K117N) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
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33428962 |
| MDCK | EC90 |
14.0 μM
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90% inhibition of influenza A/Hong Kong/1/1968 (H3N2) escape mutant M3 (HA1 D7N + HA2 K117N) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
90% inhibition of influenza A/Hong Kong/1/1968 (H3N2) escape mutant M3 (HA1 D7N + HA2 K117N) replication in canine MDCK cells measured by escape mutant viral yield reduction assay after 24 h incubation.
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33428962 |
CBS1194 (0.006-100 μM) potently and specifically inhibits the infection of A549 cells by pseudoviruses carrying group 2 influenza H7 HA, with an EC50 of 0.25 μM; it also potently and selectively inhibits the replication of group 2 influenza strains in MDCK cells, with EC50 values ranging from 0.74 μM to 3.17 μM[2].
CBS1194 inhibits the replication of the influenza reporter virus A/NY-r19-GLuc (H3N2) in MDCK cells, with an EC50 value of 0.36 μM[2].
CBS1194 (12.5 μM; administered at intervals: −1 to 0 h, −1 to 2 h, 0 to 2 h, 2 to 4 h, 4 to 6 h, 6 to 8 h, −1 to 8 h post-infection; virus yield measured at 24 h post-infection) acts during the early stage of viral entry (0 to 2 h post-infection) to inhibit the replication of influenza A virus A/Hong Kong/1/1968 (H3N2) in MDCK cells[2].
CBS1194 (0.16-40 μM; 30 min incubation with virus at room temperature, 30 min incubation with erythrocytes at 37°C, 30 min hemolysis induction at 37°C) dose-dependently inhibits the HA-mediated hemolysis of chicken erythrocytes by influenza A virus A/Hong Kong/1/1968 (H3N2), with an IC50 of 0.67 μM, and does not induce hemolysis on its own[2].
CBS1194 stabilizes the HA protein of influenza A virus A/Hong Kong/1/1968 (H3N2), rendering it resistant to low pH-induced conformational changes[2].
CBS1194 potently inhibits group 2 influenza A virus strains by blocking HA rearrangement required for membrane fusion, with an in vitro EC50 of 0.36-3.7 μM and a CC50 >100 μM[3].
CBS1194 inhibits trypsin-mediated limited cleavage of hemagglutinin protein of influenza A virus subtype H7[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CBS1194 (25-100 mg/kg, intraperitoneal injection, twice daily, administered 2 hours before infection) exerts no significant reducing effect on pulmonary bioluminescent signals (a marker of viral load) in female BALB/c mice infected with influenza A virus PR8-Fluc[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 4-6 weeks old, intranasal inoculation with sublethal dose of X31-Fluc (H3N2) reporter virus)[1]
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Dosage:25 mg/kg/day; 100 mg/kg/day
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Administration:i.p.; daily
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Result:Showed no inhibition against influenza A virus infection in vivo.
Did not reduce bioluminescence signals indicating viral load relative to untreated controls.
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Animal Model:BALB/c (female, 4-6 weeks old, intranasal infection with reporter IAV PR8-Fluc at 1,000 TCID50)[4]
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Dosage:25 mg/kg/day; 100 mg/kg/day
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Administration:i.p.; twice daily; initiated 2 hours before infection
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Result:Exhibited a mean total lung bioluminescence flux of ~2.5×107 p/s at 25 mg/kg/day, which was not significantly different from the vehicle control group.
Exhibited a mean total lung bioluminescence flux of ~2×107 p/s at 100 mg/kg/day, which was also not significantly different from the vehicle control group.
Chemical Information
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CAS. Nr. 901259-15-2
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Molecular Weight 451.32
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Formel C22H19BrN4O2
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SMILES
BrC1=CC=CC(=C1)C=2N=C3N=C(C=C(N3C2NC4=CC=C5OCCOC5=C4)C)C
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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
[2]. Du R, et al. Identification of a novel inhibitor targeting influenza A virus group 2 hemagglutinins. Antiviral research. 2021 Feb;186:105013. [Content Brief]
[3]. Chen Z, et al. Small Molecule Inhibitors of Influenza Virus Entry. Pharmaceuticals (Basel, Switzerland). 2021 Jun 18;14(6):587. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)