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Fig. 1 · Structure
Cat. No.
A14194
CAS No.
174022-42-5
Formula
C36H56O6
Mol. Weight
584.82

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Bevirimat

Cat. No. A14194 CAS 174022-42-5

HIV-1 maturation inhibitor

Bevirimat (MPC-4326, PA-457, YK-FH312) is a first-in-class HIV-1 maturation inhibitor that demonstrates high potency in cell culture and has shown clinical efficacy in HIV-1-infected patients.

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Publications for Bevirimat

1 publication citing this product

  1. Mingzhang Wang, .et al. , Nat Commun, 2017, 8: 1779 PMID: 29176596
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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
H9 EC50 < 0.00035 μM 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 Cytotoxicity against human H9 cells after 4 days by coulter counter [PMID: 20187635]
H9 IC50 7 μM Antiviral activity against HIV1 infected in human H9 cells after 4 days by p24 antigen ELISA [PMID: 20187635]
H9 IC50 7 μM 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 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 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 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 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 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 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 Cytotoxicity against MT2 cells by XTT assay [PMID: 17935987]
MT2 EC50 0.0013 μM 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 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 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 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 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 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 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 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]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 174022-42-5
Applications HIV-1 maturation inhibitor
Formula C36H56O6
Molecular Weight 584.82
Synonyms BVM,MPC-4326; PA-457
SMILES
CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]3CC[C@@H]4[C@]5(CC[C@@H](C([C@@H]5CC[C@]4([C@@]3(CC2)C)C)(C)C)OC(=O)CC(C)(C)C(=O)O)C)C(=O)O

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 90 mg/mL (153.88 mM)
Ethanol <1 mg/mL

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Publications

1 publication citing this product

  1. Mingzhang Wang, .et al. , Nat Commun, 2017, 8: 1779 PMID: 29176596

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