PF-46396
PF-46396 is a potent HIV-1 inhibitor with an EC50 value of 0.206 µM. PF-46396 shows antiviral activity. PF-46396 inhibits the processing of capsid (CA)/spacer peptide 1 (SP1) (p25) Gag precursor proteins and blocks maturation of the viral core particle.
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- CAS No.: 1207481-21-7
- Formule: C27H29F3N2O
- Masse moléculaire:454.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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HIV-1 0.206 μM (EC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CEM-SS | CC50 |
20 μM
Compound: PF-46396
|
Cytotoxicity against human CEM-SS cells after 6 days by XTT assay
Cytotoxicity against human CEM-SS cells after 6 days by XTT assay
|
[PMID: 19805571] |
| CEM-SS | EC50 |
>20 μM
Compound: PF-46396
|
Antiviral activity against HIV1 RF infected in human CEM-SS cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
Antiviral activity against HIV1 RF infected in human CEM-SS cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
|
[PMID: 19805571] |
| HeLa | EC50 |
>10 μM
Compound: PF-46396
|
Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
|
[PMID: 19805571] |
| HeLa | EC50 |
>10 μM
Compound: PF-46396
|
Antiviral activity against HIV1 NL4-3 infected in human HeLa cells assessed as decrease in single-cycle viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against HIV1 NL4-3 infected in human HeLa cells assessed as decrease in single-cycle viral infection after 72 hrs by beta-galactosidase reporter gene assay
|
[PMID: 19805571] |
| HeLa | EC50 |
>3.2 μM
Compound: PF-46396
|
Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
|
[PMID: 19805571] |
| HeLa | EC50 |
0.206 μM
Compound: PF-46396
|
Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
|
[PMID: 19805571] |
| MT2 | CC50 |
15 μM
Compound: PF-46396
|
Cytotoxicity against human MT2 cells after 6 days by XTT assay
Cytotoxicity against human MT2 cells after 6 days by XTT assay
|
[PMID: 19805571] |
| MT2 | EC50 |
>16 μM
Compound: PF-46396
|
Antiviral activity against HIV1 RF infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
Antiviral activity against HIV1 RF infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
|
[PMID: 19805571] |
| MT2 | EC50 |
0.017 μM
Compound: PF-46396
|
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
|
[PMID: 19805571] |
| MT2 | EC50 |
0.21 μM
Compound: PF-46396
|
Antiviral activity against HIV1 92HT599 infected in human MT2 cells assessed as inhibition of viral p24 antigen production after 5 days
Antiviral activity against HIV1 92HT599 infected in human MT2 cells assessed as inhibition of viral p24 antigen production after 5 days
|
[PMID: 19805571] |
| MT2 | EC50 |
0.24 μM
Compound: PF-46396
|
Antiviral activity against HIV1 92HT594 infected in human MT2 cells assessed as inhibition of viral p24 antigen production after 5 days
Antiviral activity against HIV1 92HT594 infected in human MT2 cells assessed as inhibition of viral p24 antigen production after 5 days
|
[PMID: 19805571] |
| MT2 | EC50 |
0.36 μM
Compound: PF-46396
|
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity after 6 days by XTT assay
|
[PMID: 19805571] |
Chemical Information
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CAS No. 1207481-21-7
-
Masse moléculaire 454.53
-
Formule C27H29F3N2O
-
SMILES
O=C1C(C(F)(F)F)=CC=CN1CC(NC2CC3=C(C=CC=C3)C2)C4=CC=C(C(C)(C)C)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)