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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1207481-21-7
- 分子式: C27H29F3N2O
- 分子量:454.53
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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
IC50 & Target
[1]|
HIV-1 0.206 μM (EC50) |
Cellular Effect
|
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] |
化学情報
-
CAS 番号 1207481-21-7
-
分子量 454.53
-
分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)