1. Anti-infection
  2. HIV
  3. 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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PF-46396 Chemical Structure

PF-46396 Chemical Structure

CAS No. : 1207481-21-7

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Description

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[1].

IC50 & Target[1]

HIV-1

0.206 μM (EC50)

Cellular Effect
Cell Line Type Value Description References
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]
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]
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
> 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
> 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 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]
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]
Molecular Weight

454.53

Formula

C27H29F3N2O

CAS No.
SMILES

O=C1C(C(F)(F)F)=CC=CN1CC(NC2CC3=C(C=CC=C3)C2)C4=CC=C(C(C)(C)C)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PF-46396 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PF-46396
Cat. No.:
HY-120764
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