1. Anti-infection
  2. Virus Protease
  3. Bevirimat

Bevirimat  (Synonyms: PA-457; MPC-4326; YK FH312)

Cat. No.: HY-N0842 Purity: 99.80%
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Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies.

For research use only. We do not sell to patients.

Bevirimat Chemical Structure

Bevirimat Chemical Structure

CAS No. : 174022-42-5

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Description

Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
H9 EC50
< 0.00035 μM
Compound: 2
Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound able to suppress HIV replication by 50%.
Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound able to suppress HIV replication by 50%.
[PMID: 9804704]
H9 EC50
0.00035 μM
Compound: 133, DSB, PA-457, MPC-4326
Cytotoxicity against human H9 cells after 4 days by coulter counter
Cytotoxicity against human H9 cells after 4 days by coulter counter
[PMID: 20187635]
H9 IC50
7 μM
Compound: 133, DSB, PA-457, MPC-4326
Antiviral activity against HIV1 infected in human H9 cells after 4 days by p24 antigen ELISA
Antiviral activity against HIV1 infected in human H9 cells after 4 days by p24 antigen ELISA
[PMID: 20187635]
H9 IC50
7 μM
Compound: 2
Antiviral activity against HIV1 3B isolate replication in human H9 cells assessed as decrease in viral p24 level after 4 days
Antiviral activity against HIV1 3B isolate replication in human H9 cells assessed as decrease in viral p24 level after 4 days
[PMID: 11141100]
HeLa EC50
> 1 μM
Compound: DSB
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
0.009 μM
Compound: DSB
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]
HeLa EC50
0.29 μM
Compound: DSB
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]
MT2 CC50
> 10 μM
Compound: bevirimat
Cytotoxicity against mock-infected human MT2 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer Glo assay
Cytotoxicity against mock-infected human MT2 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer Glo assay
[PMID: 25927586]
MT2 EC50
> 10000 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein delta V370 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein delta V370 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
> 10000 nM
Compound: 1
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 IC50
> 42.78 μM
Compound: 2
Cytotoxicity against MT2 cells by XTT assay
Cytotoxicity against MT2 cells by XTT assay
[PMID: 17935987]
MT2 EC50
0.0013 μM
Compound: 2, Bevirimat
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication treated 1 day after infection measured on after 4 days postinfection by p24 antigen ELISA
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication treated 1 day after infection measured on after 4 days postinfection by p24 antigen ELISA
[PMID: 20329730]
MT2 EC50
0.005 nM
Compound: PA-457
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days
[PMID: 20660667]
MT2 EC50
0.01 μM
Compound: 1; BVM
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
[PMID: 26968652]
MT2 IC50
0.01 μM
Compound: bevirimat
Antiviral activity against HIV1 NL4.3-Ren infected in human MT2 cells assessed as inhibition of viral growth measured 48 hrs post infection by luminometry
Antiviral activity against HIV1 NL4.3-Ren infected in human MT2 cells assessed as inhibition of viral growth measured 48 hrs post infection by luminometry
[PMID: 25927586]
MT2 EC50
0.011 μM
Compound: 2
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as p24 antigen level after 4 days by ELISA
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as p24 antigen level after 4 days by ELISA
[PMID: 19388685]
MT2 EC50
0.05 nM
Compound: PA-457
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days
[PMID: 20660667]
MT2 EC50
0.5 nM
Compound: PA-457
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days
[PMID: 20660667]
MT2 EC50
0.553 μM
Compound: 1; BVM
Antiviral activity against HIV1 containing gag V370A mutant infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
Antiviral activity against HIV1 containing gag V370A mutant infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
[PMID: 26968652]
MT2 EC50
0.974 μM
Compound: 1; BVM
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days in presence of 15 mg/ml HSA by luciferase report gene based multiple cycle drug susceptibility assay
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days in presence of 15 mg/ml HSA by luciferase report gene based multiple cycle drug susceptibility assay
[PMID: 26968652]
MT2 EC50
10 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
10 nM
Compound: 1
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
1114 nM
Compound: 1
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
1291 nM
Compound: 1
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 CC50
16.8 μM
Compound: 1; BVM
Cytotoxicity against human MT2 cells assessed as cell viability by redox dye assay
Cytotoxicity against human MT2 cells assessed as cell viability by redox dye assay
[PMID: 26968652]
MT2 EC50
1810 nM
Compound: 2; BVM
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein V370M mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein V370M mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
1810 nM
Compound: 1
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
34 nM
Compound: BVM
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT-2 cells by XTT-assay
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT-2 cells by XTT-assay
[PMID: 20308382]
MT2 EC50
40 nM
Compound: 2; BVM
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein T371A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein T371A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
40 nM
Compound: 1
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 CC50
40 μM
Compound: 2
Cytotoxicity against human MT2 cells by XTT assay
Cytotoxicity against human MT2 cells by XTT assay
[PMID: 19388685]
MT2 IC50
42.78 μM
Compound: 2, Bevirimat
Cytotoxicity against human MT2 cells by XTT assay
Cytotoxicity against human MT2 cells by XTT assay
[PMID: 20329730]
MT2 EC50
552 nM
Compound: 1
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
553 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein V370A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein V370A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
7 nM
Compound: 1
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
74 nM
Compound: 1
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
77 nM
Compound: 2; BVM
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein delta T371 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein delta T371 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
77 nM
Compound: 1
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
974 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay in presence of human serum albumin
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay in presence of human serum albumin
[PMID: 26988305]
MT4 CC50
> 10 μM
Compound: 1
Cytotoxicity against human MT4 cells for 4 days
Cytotoxicity against human MT4 cells for 4 days
[PMID: 23379607]
MT4 CC50
> 17 μM
Compound: 1; DSB
Cytotoxicity against human MT4 cells by cell-titer Glo assay
Cytotoxicity against human MT4 cells by cell-titer Glo assay
[PMID: 26598461]
MT4 CC50
> 2 μM
Compound: 3
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 2 days by CytoTox-Glo cytotoxicity assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 2 days by CytoTox-Glo cytotoxicity assay
[PMID: 33639343]
MT4 EC50
> 4 μM
Compound: BVM
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 EC50
> 4 μM
Compound: BVM
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaT371 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaT371 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
[PMID: 22818973]
MT4 EC50
> 4 μM
Compound: BVM
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaV370 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaV370 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
[PMID: 22818973]
MT4 CC50
> 4.5 μM
Compound: 2
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 2 days by CytoTox-Glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 2 days by CytoTox-Glo assay
[PMID: 27676157]
MT4 IC50
> 5 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370A mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370A mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
> 5 μM
Compound: 2
Cytotoxicity against human MT4 cells after 4 days
Cytotoxicity against human MT4 cells after 4 days
[PMID: 20673723]
MT4 IC50
> 6.8 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V362I mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V362I mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
> 6.8 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag T371 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag T371 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
> 6.8 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 CC50
> 6.84 μM
Compound: 3; DSB
Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay
Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay
[PMID: 33214842]
MT4 IC50
0.065 μM
Compound: 2
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by p24 ELISA
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by p24 ELISA
[PMID: 27676157]
MT4 EC50
0.075 μM
Compound: 1; DSB
Antiviral activity against HIV-1 NL4-3 infected in MT4 cells assessed inhibition of viral replication measured on day 4 postinfection by ELISA
Antiviral activity against HIV-1 NL4-3 infected in MT4 cells assessed inhibition of viral replication measured on day 4 postinfection by ELISA
[PMID: 26598461]
MT4 EC50
0.076 μM
Compound: BVM
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 IC50
0.076 μM
Compound: 1
Antiviral activity against 0.001 MOI wild type Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI wild type Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
0.087 μM
Compound: 2, Bervirimat, DSB, MPC-4326
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as p24 antigen level after 4 days by ELISA
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as p24 antigen level after 4 days by ELISA
[PMID: 22978745]
MT4 EC50
0.096 μM
Compound: 2
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 4 days by p24 antigen based ELISA assay
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 4 days by p24 antigen based ELISA assay
[PMID: 20673723]
MT4 CC50
14.2 μM
Compound: 2, Bervirimat, DSB, MPC-4326
Cytotoxicity against human MT4 cells after 2 days
Cytotoxicity against human MT4 cells after 2 days
[PMID: 22978745]
MT4 IC50
15.2 μM
Compound: PA-457
Cytotoxicity against human MT4 lymphocytes after 48 hrs by MTT assay
Cytotoxicity against human MT4 lymphocytes after 48 hrs by MTT assay
[PMID: 21123066]
MT4 CC50
15.9 μM
Compound: DSB
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescent assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescent assay
[PMID: 30703659]
MT4 IC50
7.71 μM
Compound: 2
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring GagV370A mutant infected in human MT4 cells by p24 ELISA
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring GagV370A mutant infected in human MT4 cells by p24 ELISA
[PMID: 27676157]
THP-1 IC50
54 μM
Compound: 25, bevirimat
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by AlamarBlue assay
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by AlamarBlue assay
10.1039/C3MD00282A
In Vitro

Bevirimat inhibits wild-type HIV-1 replication with a mean IC50 of 10.3 nM[2].
Bevirimat (72 h) shows antiviral activity against wild type HIV1 and HIV1 harboring capsid I201V mutant protein infected in human HeLa cells, with a EC50 of 0.009 and 0.29 μM[3].
Bevirimat (48 h) shows cytotoxicity against mock-infected human MT2 cells, with a CC50 of > 10 μM[4].
Bevirimat (1 day) shows antiviral activity against HIVIIIB infected in human MT2 cells assessed as inhibition of viral replication, with a EC50 of 0.0013 μM[5].
Bevirimat (48 h) shows cytotoxicity against human MT4 cells assessed as reduction in cell viability by CytoTox-Glo cytotoxicity assay, with a CC50 of > 2 μM[6].
Bevirimat (4 days) shows antiviral activity against HIV1NL4-3 infected in human MT4 cells assessed as p24 antigen level, with a IC50 of 0.087 μM[7].
Bevirimat (3 days) shows cytotoxicity against HIV-1-infected C8166 cells, with a mean CC50 of 53.23 μM[9].
Bevirimat (0-8 μM, 3 days) has a weak inhibitory effect on the replication of HIV-1IIIB in C8166 cells in the presence of 20% human serum[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bevirimat (10-100 mg/kg, p.o., twice-daily, 22 days) potently inhibits HIV-1 replication and prevents thymocyte depletion in SCID-hu Thy/Liv mice[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C.B-17 SCID-hu Thy/Liv mice (implanted with tissues from a single donor; implants were inoculated 18 weeks after implantation with 50 µL of stock virus (500–2,000 50% tissue-culture infectious doses) or RPMI 1640 medium (mock infection) by direct injection)[8]
Dosage: 10, 30, and 100 mg/kg
Administration: Oral gavage (p.o.), beginning 1 day before inoculation by direct injection of the Thy/Liv implants and continuing until implant collection 21 days after inoculation
Result: Inhibited viral replication in a dose-dependent manner, reducing implant HIV-1 RNA by 2.1 log10 copies, p24 by 96%, and Gag-p24+ thymocytes from 7% to <1% at 100 mg/kg per day when compared with untreated mice.
Caused significant protection of the implants from virus-mediated loss of cellularity at 10 and 30 mg/kg per day, from depletion of CD4+CD8+ thymocytes at 100 mg/kg per day, and from a reduction in CD4/CD8 ratio at 30 and 100 mg/kg per day.
Clinical Trial
Molecular Weight

584.83

Formula

C36H56O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC([C@]1(CC[C@H]2C(C)=C)[C@@]2([H])[C@](CC[C@@]3([H])[C@]4(CC[C@]5([H])[C@@]3(CC[C@H](OC(CC(C)(C)C(O)=O)=O)C5(C)C)C)C)([H])[C@@]4(C)CC1)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (85.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7099 mL 8.5495 mL 17.0990 mL
5 mM 0.3420 mL 1.7099 mL 3.4198 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.27 mM); Suspended solution; Need ultrasonic and warming

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.80%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7099 mL 8.5495 mL 17.0990 mL 42.7475 mL
5 mM 0.3420 mL 1.7099 mL 3.4198 mL 8.5495 mL
10 mM 0.1710 mL 0.8549 mL 1.7099 mL 4.2747 mL
15 mM 0.1140 mL 0.5700 mL 1.1399 mL 2.8498 mL
20 mM 0.0855 mL 0.4275 mL 0.8549 mL 2.1374 mL
25 mM 0.0684 mL 0.3420 mL 0.6840 mL 1.7099 mL
30 mM 0.0570 mL 0.2850 mL 0.5700 mL 1.4249 mL
40 mM 0.0427 mL 0.2137 mL 0.4275 mL 1.0687 mL
50 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8549 mL
60 mM 0.0285 mL 0.1425 mL 0.2850 mL 0.7125 mL
80 mM 0.0214 mL 0.1069 mL 0.2137 mL 0.5343 mL
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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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