Bevirimat
Based on 2 publication(s) in Google Scholar
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.
- Purity: 99.82%
- CAS No.: 174022-42-5
- Formula: C36H56O6
- Molecular Weight:584.83
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Bevirimat
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Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
| H9 | EC50 |
<0.00035 μM
Compound: 2
|
Cytotoxicity against mock-infected human H9 cells
Cytotoxicity against mock-infected human H9 cells
|
[PMID: 11141100] |
| H9 | EC50 |
<0.35 nM
Compound: 2
|
Cytotoxicity against mock-infected human H9 cells
Cytotoxicity against mock-infected human H9 cells
|
[PMID: 11141100] |
| H9 | EC50 |
<0.00035 μM
Compound: 2
|
Evaluated for the anti-HIV activity against HIV-1 replication in H9 lymphocyte cells
Evaluated for the anti-HIV activity against HIV-1 replication in H9 lymphocyte cells
|
[PMID: 11206454] |
| H9 | EC50 |
<0.35 nM
Compound: 2
|
Evaluated for the anti-HIV activity against HIV-1 replication in H9 lymphocyte cells
Evaluated for the anti-HIV activity against HIV-1 replication in H9 lymphocyte cells
|
[PMID: 11206454] |
| H9 | IC50 |
7 μM
Compound: 2 (PA-457)
|
Concentration required to produce 50% toxicity against mock-infected H9 cells
Concentration required to produce 50% toxicity against mock-infected H9 cells
|
[PMID: 15501054] |
| H9 | EC50 |
0.007 μM
Compound: 8
|
Antiviral activity against HIV1 3B in H9 lymphocytes
Antiviral activity against HIV1 3B in H9 lymphocytes
|
[PMID: 16942019] |
| H9 | IC50 |
>42.8 μM
Compound: 8
|
Cytotoxicity against human H9 lymphocytes
Cytotoxicity against human H9 lymphocytes
|
[PMID: 16942019] |
| 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 | 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 | EC50 |
0.35 nM
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 | EC50 |
>3.5 x 10-4 μM
Compound: 2, DSB, PA-457
|
Antiviral activity against HIV infected in H9 cells
Antiviral activity against HIV infected in H9 cells
|
[PMID: 23399723] |
| H9 | EC50 |
0.35 nM
Compound: 1; BVM
|
Antiviral activity against HIV1 infected in human H9 cells
Antiviral activity against HIV1 infected in human H9 cells
|
[PMID: 26968652] |
| H9 | EC50 |
<3.5 μM
Compound: 3
|
Toxic concentration on HIV-1 mock infected H9 lymphocyte cells
Toxic concentration on HIV-1 mock infected H9 lymphocyte cells
|
[PMID: 8676334] |
| H9 | IC50 |
7 μM
Compound: 3
|
Inhibitory activity against HIV-1 replication in mock infected H9 cells
Inhibitory activity against HIV-1 replication in mock infected H9 cells
|
[PMID: 8676334] |
| H9 | IC50 |
>7 μM
Compound: 2
|
Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound toxic to 50% of mock-infected H9 cells.
Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound toxic to 50% of mock-infected H9 cells.
|
[PMID: 9804704] |
| 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 |
<0.35 nM
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: 3, bevirimat, DSB, PA-457
|
Antiviral activity against Human immunodeficiency virus 1 infected human H9 cells assessed as inhibition of viral replication
Antiviral activity against Human immunodeficiency virus 1 infected human H9 cells assessed as inhibition of viral replication
|
10.1007/s00044-010-9467-2 |
| H9 | EC50 |
0.35 nM
Compound: 3, bevirimat, DSB, PA-457
|
Antiviral activity against Human immunodeficiency virus 1 infected human H9 cells assessed as inhibition of viral replication
Antiviral activity against Human immunodeficiency virus 1 infected human H9 cells assessed as inhibition of viral replication
|
10.1007/s00044-010-9467-2 |
| 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 | IC50 |
>42.78 μM
Compound: 2
|
Cytotoxicity against MT2 cells by XTT assay
Cytotoxicity against MT2 cells by XTT assay
|
[PMID: 17935987] |
| 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 | 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 |
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 |
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 | 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 |
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 |
0.05 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 | 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 | 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 | 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 |
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 | 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 | CC50 |
17 μM
Compound: 2; BVM
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 26988305] |
| 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 |
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 |
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 |
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 |
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 |
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] |
| 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 | CC50 |
16.8 nM
Compound: 1
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 27326328] |
| 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 | 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 |
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 | 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 |
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: 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 |
>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 | CC50 |
17 μM
Compound: 1; BVM
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 29631960] |
| MT2 | CC50 |
16.8 μM
Compound: 1; BVM
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 33508465] |
| MT2 | CC50 |
17 μM
Compound: 2
|
Cytotoxicity against human MT2 cells assessed as reduction in cell viability
Cytotoxicity against human MT2 cells assessed as reduction in cell viability
|
[PMID: 36441509] |
| MT4 | EC50 |
0.096 μM
Compound: 8
|
Antiviral activity against HIV1 NL4-3 in MT4 cells
Antiviral activity against HIV1 NL4-3 in MT4 cells
|
[PMID: 16942019] |
| MT4 | EC50 |
0.096 μM
Compound: 8
|
Antiviral activity against HIV1 NL4-3 replication in human MT4 cells
Antiviral activity against HIV1 NL4-3 replication in human MT4 cells
|
[PMID: 16942019] |
| MT4 | EC50 |
0.43 μM
Compound: 8
|
Antiviral activity against HIV1 PI-R replication in human MT4 cells
Antiviral activity against HIV1 PI-R replication in human MT4 cells
|
[PMID: 16942019] |
| MT4 | IC50 |
>5 μM
Compound: 8
|
Cytotoxicity against human MT4 cells at 5 uM
Cytotoxicity against human MT4 cells at 5 uM
|
[PMID: 16942019] |
| 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 | 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 |
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 | 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 | 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 |
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 | 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 |
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 | CC50 |
>10 μM
Compound: 1
|
Cytotoxicity against human MT4 cells for 4 days
Cytotoxicity against human MT4 cells for 4 days
|
[PMID: 23379607] |
| 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 |
>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 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 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 | 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 | 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 | 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 | 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 |
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 | 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] |
| 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 | 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 | 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] |
| Raji | IC50 |
396 molar ratio
Compound: 3
|
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction after 48 hrs relative to TPA
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction after 48 hrs relative to TPA
|
[PMID: 19481937] |
| Raji | IC50 |
396 molar ratio
Compound: Bevirimat
|
Chemopreventive activity in human Raji cells assessed as molar ratio of compound required to inhibit 50% of control of inhibition of TPA-induced EBV-early antigen activation after 48 hrs by immunofluorescence analysis
Chemopreventive activity in human Raji cells assessed as molar ratio of compound required to inhibit 50% of control of inhibition of TPA-induced EBV-early antigen activation after 48 hrs by immunofluorescence analysis
|
[PMID: 24411124] |
| 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 |
| TZM | EC50 |
>17.1 μM
Compound: 8
|
Inhibition of membrane fusion between HIV1 NL4-3 envelope gene expressing COS cells and TZM cells
Inhibition of membrane fusion between HIV1 NL4-3 envelope gene expressing COS cells and TZM cells
|
[PMID: 16942019] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:10, 30, and 100 mg/kg
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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
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 174022-42-5
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Appearance Solid
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Molecular Weight 584.83
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Formula C36H56O6
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Color White to off-white
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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
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Synonyms
PA-457; MPC-4326; YK FH312
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Vet Microbiol
The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]2026 May:316:110992. PMID: 41865607
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Martin DE, et al. Bevirimat: a novel maturation inhibitor for the treatment of HIV-1 infection. Antivir Chem Chemother. 2008;19(3):107-13. [Content Brief]
[2]. Li F, et al. PA-457: a potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing. Proc Natl Acad Sci U S A. 2003 Nov 11;100(23):13555-60. [Content Brief]
[3]. Blair WS, et al. New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. Antimicrob Agents Chemother. 2009 Dec;53(12):5080-7. [Content Brief]
[4]. Callies O, et al. Isolation, Structural Modification, and HIV Inhibition of Pentacyclic Lupane-Type Triterpenoids from Cassine xylocarpa and Maytenus cuzcoina. J Nat Prod. 2015 May 22;78(5):1045-55. [Content Brief]
[5]. Qian K, et al. Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. J Med Chem. 2010 Apr 22;53(8):3133-41. [Content Brief]
[6]. Zhao Y, et al. Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors. Eur J Med Chem. 2021 Apr 5;215:113287. [Content Brief]
[7]. Qian K, et al. Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. J Med Chem. 2012 Sep 27;55(18):8128-36. [Content Brief]
[8]. Stoddart CA, et al. Potent activity of the HIV-1 maturation inhibitor bevirimat in SCID-hu Thy/Liv mice. PLoS One. 2007 Nov 28;2(11):e1251. [Content Brief]
[9]. Zhao L, et al. Pre-clinical pharmacological profile of QF-036, a potent HIV-1 maturation inhibitor. Basic Clin Pharmacol Toxicol. 2021 Feb;128(2):275-285. [Content Brief]
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 |