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 番号: 901259-15-2
- 分子式: C22H19BrN4O2
- 分子量:451.32
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | EC50 |
0.25 μM
|
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.
|
33428962 |
| A549 | CC50 |
100 μM
Compound: 5; CBS1194
|
Cytotoxicity against human A549 cells incubated for 48 hrs by celltiter-glo luminescent cell viability assay
Cytotoxicity against human A549 cells incubated for 48 hrs by celltiter-glo luminescent cell viability assay
|
[PMID: 36260129] |
| A549 | EC50 |
49.30 μM
|
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.
|
33428962 |
| A549 | EC50 |
54.53 μM
|
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.
|
33428962 |
| MDCK | EC50 |
3.17 μM
|
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.
|
33428962 |
| MDCK | EC50 |
1.60 μM
|
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.
|
33428962 |
| MDCK | EC50 |
0.74 μM
|
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.
|
33428962 |
| MDCK | EC50 |
0.36 μM
|
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.
|
33428962 |
| MDCK | EC90 |
2.8 μM
|
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.
|
33428962 |
| MDCK | EC90 |
13.3 μM
|
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.
|
33428962 |
| MDCK | EC90 |
17.4 μM
|
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.
|
33428962 |
| MDCK | EC90 |
14.0 μM
|
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.
|
33428962 |
体外実験
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. Further protocols information, click here.
体内実験
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.
化学情報
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CAS 番号 901259-15-2
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分子量 451.32
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分子式 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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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]. Lin X, et al. Optimization and applications of an in vivo bioluminescence imaging model of influenza A virus infections. Virologica Sinica. 2023 Aug;38(4):631-634. [Content Brief]
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)